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FYARRO Sirolimus 5 mg/mL Injection, Powder, Lyophilized, For Suspension — NDC 80803-0153-50 package photo
Label image from the product's FDA listing (DailyMed) — may show a different pack size or an older label revision.

FYARRO Sirolimus 5 mg/mL Injection, Powder, Lyophilized, For Suspension — NDC 80803-153-50 (Billing 80803-0153-50)

by Aadi Bioscience, Inc. · 1 VIAL, SINGLE-USE in 1 CARTON / 20 mL in 1 VIAL, SINGLE-USE

This is a package of FYARRO Sirolimus 5 mg/mL Injection, Powder, Lyophilized, For Suspension from Aadi Bioscience, Inc., marketed since Dec 2021 and currently FDA-listed. It is this product's only package size.

NDC 80803-0153-50
🏷️ FDA NDC (as labeled) 80803-153-50 billing pads the product segment with a zero
Rx only Brand On market Non-controlled ⇄ Compare with another NDC
🗂️ FDA directory synced Oct 1, 2026 · this listing last changed Oct 1, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →
⚠️
Other active recalls for Sirolimus (different manufacturers) — 1 · tap to view
These affect other manufacturers’ products for the same ingredient — not necessarily the exact NDC on this page.
Class III · May 1, 2024 — Failed Impurities/Degradation Specifications (Dr. Reddy's Laboratories, Inc.) · FDA recall D-0504-2024
Each entry is an official FDA enforcement report — look up any recall number in the FDA recall database ↗
Past resolved recalls for this product (1)
Class III · Oct 13, 2022 · Terminated — Failed Stability Specifications (Aadi Bioscience) · FDA recall D-0059-2023

Identity & classification

Regulatory identifiers FDA, NLM and CMS codes for this package

FDA NDC (as labeled) 80803-153-50
Product NDC 80803-153
11-digit billing NDC 80803015350
NCPDP billing unit EA — each (per item)
Application # NDA213312
SPL Set ID 0f9bb784-53e2-46f9-a65d-1c6c2a230eaf
Established class (EPC) Kinase Inhibitor; mTOR Inhibitor Immunosuppressant
Mechanism of action Protein Kinase Inhibitors; mTOR Inhibitors
Physiologic effect Decreased Immunologic Activity
DEA schedule Non-controlled
Marketing category NDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2021-12-06
Route INTRAVENOUS
Dosage form INJECTION, POWDER, LYOPHILIZED, FOR SUSPENSION
Substance SIROLIMUS

Drug-database identifiers Medi-Span GPI and First Databank GCN / HICL / AHFS classification

GCN Seq No 082845
GCN 51562
HICL code 047680
Ingredient (HICL) Sirolimus Protein-Bound
HIC1 code V
Therapeutic class — broad (HIC1) Neoplasms
HIC2 code V3
Therapeutic class — intermediate (HIC2) Antineoplastic Drugs (Continued 1)
HIC3 code V3C
Therapeutic class — specific (HIC3) Antineoplastic - Mtor Kinase Inhibitors
AHFS code 10:00.00.00
AHFS class Antineoplastic Agents
FDB label name FYARRO 100 MG VIAL
FDB brand name Fyarro
Legend status F — Federal legend — prescription drug or device
Quick answers
  • GSN (GCN sequence number): 082845
  • GCN: 51562
  • HICL (First Databank): 047680
  • AHFS class code: 10:00.00.00
Why two NDCs? The FDA registers this code as 80803-153-50 — a 5-3-2 layout, and that's what's printed on the package and shown on DailyMed. For insurance claims, every NDC is standardized to a uniform 11-digit 5-4-2 format by adding a zero to the product segment → 80803-0153-50. Same drug, same package — only the format differs.
Where does this data come from?
Identifiers from the FDA openFDA NDC Directory and Structured Product Labeling; RxCUI from RxNorm (NLM); GPI from Medi-Span; GCN / HIC / AHFS / legend from First Databank.

Clinical

Label name FYARRO 100 MG VIAL Ingredient Sirolimus Protein-Bound
📖 What it is MedlinePlus · NLM

Sirolimus (with albumin) injection is used to treat a certain type of epithelioid cell tumor (soft tissue cancer that can form in any part of the body). Sirolimus is in a class of medications called kinase inhibitors. It works by blocking the action of the abnormal protein that tells the cancer cells to multiply. This may help slow the growth of tumors.

Read the full MedlinePlus article ↗
📗 Our plain-language guide HelloPharmacist
  • Oral sirolimus helps prevent your body from rejecting a transplanted kidney if you are 13 or older. It is also used for LAM, a rare lung disease. Other sirolimus products treat a t...
  • Take oral sirolimus once a day, the same way each time, either always with food or always without. Swallow tablets whole and do not crush, chew or split them. Never take it with gr...
  • Swelling, high blood pressure, high cholesterol, stomach upset, headache and acne are common. Call your doctor right away for fever or other signs of infection, new cough or troubl...
  • What side effects are normal, and when should I call?
📖 Read our full Sirolimus guide →
Where does this data come from?
Plain-language summary from MedlinePlus (U.S. National Library of Medicine); supplement & herbal interactions and nutrient depletion data from the Natural Medicines database; our full guide is HelloPharmacist editorial content.

Pricing

A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.

Price systemPer mLPer package
Retail pharmacies payNADAC · weekly Not in the retail survey — common for institutional, discontinued, or low-volume packs.
Medicaid paysCMS SDUD · 12 mo $6,350.11 $127,002.17 / 20 ml
Medicare drug plans payPart D · quarterly No Part D plan price is available for this NDC in our data.
Medicare Part B allowsASP · J9331 $91.030 / J9331 unit —
Where does this data come from?
NADAC (National Average Drug Acquisition Cost) is the CMS weekly pharmacy-acquisition-cost survey — what pharmacies pay. ASP (Average Sales Price) is the CMS Medicare Part B drug-payment file, published quarterly. Medicaid pays is computed by us from CMS State Drug Utilization Data (total reimbursed ÷ units, trailing 12 months) — gross of rebates and inclusive of dispensing fees, so it reflects what Medicaid paid, not an acquisition cost. Medicare drug plans pay is the median negotiated point-of-sale unit cost across plans listing this NDC in the CMS quarterly Prescription Drug Plan pricing files, before rebates. The VA pays is the federal contract price (FSS, and the statutory Big 4 ceiling where listed) from the VA National Acquisition Center pharmaceutical price file. All are free public government data; each measures a different payer, so the figures are not directly comparable.

Billing & reimbursement

FDA NDC (as labeled)80803-153-50
11-digit billing NDC80803-0153-50
Format5-3-2 as registered → padded to 5-4-2 for billing (zero added to the product segment)
HCPCS J-codeJ9331
DescriptorInjection, sirolimus protein-bound particles, 1 mg
Billing units / pkg100 units
How the units are derivedThis package is 1; the HCPCS unit is 1 MG, so one package = 100 billing units.
Medicare Part B spend (2026 (Q1))$2,400,501 · 150 claims · $16,003.34 per claim (all NDCs under J9331)
Crosswalk sourceCMS ASP NDC-HCPCS Crosswalk
Where does this data come from?
The HCPCS J-code crosswalk comes from the CMS ASP NDC-HCPCS crosswalk and the DMEPDAC (DME MAC) NDC-HCPCS crosswalk — free public CMS data. Billing units are derived from the code’s descriptor and the package amount.

Packaging — all sizes for this product

Package NDCDescription Marketing startMarketing endStatus
80803-0153-50 You're viewing this Main listing 1 VIAL, SINGLE-USE in 1 CARTON / 20 mL in 1 VIAL, SINGLE-USE 2021-12-06 — Active

Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Fyarro 5 mg/mLthis 80803-0153-50 Aadi 1 vial — — FDA listed —
About this product: this is the brand-name version. We did not find an FDA-approved generic match for this exact strength, form and route.
Where does this data come from?
Equivalents are other NDCs of the same ingredient, form and route from the openFDA NDC Directory, ranked least-expensive-first by NADAC. Therapeutic-equivalence (AB) ratings come from the FDA Orange Book; biologics use the FDA Purple Book for biosimilar & interchangeable status.

Availability & generic status

🏛️
2021
First FDA approval
Nov 2021
📍
2026
Currently FDA-listed
5 years listed
🛡️
2040
Latest patent/protection listed
not a guaranteed launch date
🔒No FDA-approved generic found

We did not find an FDA-approved generic match for this exact strength, form and route. Patent/protection dates below may affect future generic timing.

🛡️ Latest patent/protection date listed: FDA patent/protection data lists protections through Oct 2040. This may affect when a full generic version becomes widely available, but it is not a guaranteed launch date.
📅 FDA approved Nov 22, 2021 RLD RS ⏳ ~14.1 yr to latest listed protection

Why the date isn’t exact: Generic timing can change because patents may be challenged, settled, licensed, added, removed, or worked around with a narrower label — and FDA approval does not always mean a pharmacy can get the generic today.

Patents & exclusivity — FDA Orange Book
US 12133844 — method of use (U-4040)
US 12133844 — method of use (U-4041)
US 12133844 — method of use (U-4042)
US 10973806 — method of use (U-3258)
US 8911786 — method of use (U-3259)
US 10206887 — drug product
US 11497737 — drug product
US 12061183 — drug product
US 10705070 — drug product
Exclusivity ODE-386
2021 2023 2025 2027 2029 2031 2033 2035 2037 2039
Today
LOE
Substance patent Formulation patent Method-of-use patent Exclusivity Pediatric +6mo
🏛️FDA exclusivity
FDA-granted marketing protection. It’s separate from patents and may be shorter than patent protection.
🧪Product / substance patents
Patents covering the active ingredient, product, formulation, or related drug features.
🎯Method-of-use patents
Patents covering specific approved uses. These can sometimes be carved out with a “skinny label,” but not always.
🛈 What do these terms mean?
Patent
Legal protection listed in the Orange Book that may delay generic approval or launch. Issued by the U.S. Patent & Trademark Office.
Substance patent
Covers the active drug molecule itself — the hardest to design around. A generic generally can’t launch until it expires.
Formulation (product) patent
Covers a specific formulation or dosage form. A generic can sometimes work around it with a different formulation.
Method-of-use patent
A patent covering one specific approved use of the drug — not necessarily the whole molecule. A generic can sometimes launch with a “skinny label” that carves out the protected use and keeps the others.
Skinny label
A generic label that omits a still-patented use when the FDA allows it — letting a generic reach the market for the unprotected uses.
Exclusivity
FDA-granted marketing protection, separate from patents — e.g. 5-yr new chemical entity, 7-yr orphan drug, or a +6-month pediatric extension.
Paragraph IV
A generic applicant’s formal challenge to a listed patent. It can potentially lead to earlier generic entry, but often involves litigation or a settlement.
RLD / RS
Reference Listed Drug — the brand product the FDA uses as the reference for generic applications. Reference Standard — the product the FDA expects generics to compare against in bioequivalence testing.
TE / AB rating
FDA therapeutic-equivalence rating. An AB rating generally means the FDA considers a generic therapeutically equivalent to — and substitutable for — the brand.
LOE (loss of exclusivity)
The latest patent or exclusivity currently listed — the loss-of-exclusivity / latest-listed-protection date shown on this page. Paragraph-IV challenges and settlements can move the real date earlier; FDA approval and a manufacturer’s decision to market can move it later.

Built from the FDA Orange Book. The bars above are scaled to each protection’s expiry; the red LOE marker is the last one to lapse.

Listed patents (9)
PatentTypeUse codeExpires
US 12133844 ↗ Method of use U-4040 Jun 29, 2036
US 12133844 ↗ Method of use U-4041 Jun 29, 2036
US 12133844 ↗ Method of use U-4042 Jun 29, 2036
US 10973806 ↗ Method of use U-3258 Jun 29, 2036
US 8911786 ↗ Method of use U-3259 Feb 14, 2029
US 10206887 ↗ Drug product — Apr 15, 2030
US 11497737 ↗ Drug product — Oct 28, 2040
US 12061183 ↗ Drug product — Mar 5, 2036
US 10705070 ↗ Drug product — Mar 5, 2036
FDA exclusivity
CodeWhat it grantsExpires
ODE-386Orphan Drug Exclusivity (7-year)Nov 22, 2028
Common questions
Is there a generic version of FYARRO 100 MG VIAL?
No FDA-approved generic equivalent is currently listed in the FDA Orange Book for FYARRO 100 MG VIAL. Based on the patents and exclusivity currently listed, the Orange Book estimate is that full-label generic entry may be delayed until Oct 2040 — an estimate, not a guaranteed launch date.
The FDA approved a generic — why can’t I get it at my pharmacy yet?
FDA approval and pharmacy availability are two different things. The FDA can approve a generic years before it actually reaches pharmacies, because the brand company may still hold patents or have a settlement that delays the launch. A manufacturer also has to choose to make and sell it, and have supply ready. So a drug can be “FDA-approved generic exists” and still be brand-only at the counter today.
Why do different websites show different generic release dates?
Generic availability is not based on one single date. Some sources use the first exclusivity expiration, some use the last product patent, and others use the latest method-of-use patent. Patent challenges, settlements, licenses, and label carve-outs can also change the real-world launch date. This page shows the underlying Orange Book dates so you can see why estimates may differ.
What does “FDA listed” mean?
It means the product appears in the FDA’s official NDC directory. That’s a good sign a product exists and is intended for the U.S. market, but on its own it does not confirm a pharmacy can fill it today. Where we have recent retail pricing data (NADAC) for a product, we label it “Availability likely” instead.
What does a patent or protection date mean here?
It’s the latest date currently listed in the FDA Orange Book for a patent or exclusivity on the brand product. It can affect when a full generic version becomes widely available — but it is not a guaranteed generic launch date. Generics sometimes arrive earlier (through a settlement or patent challenge) or later (a manufacturer still has to make and sell one).
What does “current Orange Book estimate” mean?
It means we are using the latest patent and exclusivity dates currently listed in the FDA Orange Book. It is not a guaranteed launch date.
Can a generic come out before the last patent expires?
Sometimes. A generic company may challenge a patent, settle with the brand manufacturer, receive a license, or obtain approval with a narrower label that avoids a patented use. In other cases, the last listed protection may delay full-label generic competition.
Can a generic come out after the listed dates?
Yes. Even after patents or exclusivity expire, a generic still needs FDA approval and a manufacturer must choose to market it. Supply, litigation, business decisions, or regulatory issues can delay actual availability.
What is the difference between patents and exclusivity?
Patents are legal protections usually issued by the U.S. Patent and Trademark Office. FDA exclusivity is marketing protection granted by the FDA. They are separate, and either one can affect generic timing.
Why are there multiple patent dates?
One drug can have several patents covering different things: the active ingredient, a formulation, a manufacturing process, or a specific approved use. That is why a page may show several expiration dates instead of one simple generic date.
Built from FDA Orange Book patent and exclusivity data. Dates are refreshed from public FDA data when available; the marker is max(latest patent expiry, latest exclusivity expiry). Paragraph-IV settlements and first-filer 180-day exclusivity can shift the real date; a method-of-use patent may allow an earlier skinny-label generic for non-protected indications. Generic launch timing is an estimate, not a guarantee.
Where does this data come from?
Patents and exclusivity from the FDA Orange Book (small-molecule drugs), refreshed from public FDA data. Generic launch timing is an estimate, not a guarantee.

What it looks like

Color White
One label can cover several strengths, so colors may be combined — always confirm a loose pill against the dispensed prescription label or a pharmacist.
Where does this data come from?
Physical description (imprint, shape, color, scoring, coating) from this product’s FDA Structured Product Labeling (SPL), mirrored from DailyMed / openFDA.

Inactive Ingredients / Excipients

Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.

💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.

  • UNII ZIF514RVZR
    A protein derived from human blood plasma. In medicines, it acts as a stabilizer and binder, helping maintain drug potency and form, and may improve how the medication disperses or dissolves in the body.

1 inactive ingredient listed in the exact product block matched to this NDC.

Where does this data come from?
Data sourced from official FDA Structured Product Labeling (SPL) via DailyMed — ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.

Inactive ingredient FAQ

Are inactive ingredients the same for every manufacturer?
No. Inactive ingredients can differ by manufacturer, dosage form, strength, and package / product version.
Why might an inactive ingredient be missing?
Some SPLs do not provide a complete structured inactive-ingredient list, and older or unusual labels may only include the information in narrative text.
Can inactive ingredients matter?
Yes. They can matter for allergies, intolerances, dyes, gluten / lactose concerns, preservatives, and formulation differences — but confirm with a pharmacist or the manufacturer when it’s clinically important.

Manufacturer & labeler

LabelerAadi Bioscience, Inc.
Application holderAADI BIOSCIENCES INC
FDA applicationNDA213312 (NDA)
Labeler code80803
First marketedDec 2021
Product typeHuman Prescription Drug
The labeler markets the product; the application holder owns the FDA approval. They’re often the same company but can differ (e.g. a repackager or an authorized generic). A mailing address / phone appears here when the manufacturer includes it in the product’s FDA label (not all do).
Where does this data come from?
Labeler, application holder and registered establishment from the FDA openFDA NDC Directory and Drugs@FDA; address/contact from the product’s FDA label.

Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Very long sections are excerpted here and marked; the full text is on DailyMed (linked in the sources below). Jump with a chip, search within the label, or expand everything.
🎯 Indications and Usage 53 words ▾

1 INDICATIONS AND USAGE FYARRO ® is indicated for the treatment of adult patients with locally advanced unresectable or metastatic malignant perivascular epithelioid cell tumor (PEComa). FYARRO is an mTOR inhibitor indicated for the treatment of adult patients with locally advanced unresectable or metastatic malignant perivascular epithelioid cell tumor (PEComa). ( 1 )

⏱️ Dosage and Administration ~3 min read ▾

2 DOSAGE AND ADMINISTRATION The recommended dosage of FYARRO is 100 mg/m 2 administered as an IV infusion over 30 minutes on Days 1 and 8 of each 21-day cycle until disease progression or unacceptable toxicity. ( 2.1 )

2.1Recommended Dosage The recommended dosage of FYARRO is 100 mg/m 2 administered as an intravenous infusion over 30 minutes on Days 1 and 8 of each 21-day cycle until disease progression or unacceptable toxicity.

2.2Dosage Modifications for Adverse Reactions Table 1 lists the recommended dose reductions of FYARRO for adverse reactions. Table 1. Recommended dose reductions of FYARRO for adverse reactions. *Permanently discontinue FYARRO in patients who are unable to tolerate FYARRO after three dose reductions.

Dose Reduction Dose First Dose Reduction 75 mg/m 2 (25% reduction from 100 mg/m 2 ) Second Dose Reduction 56 mg/m 2 (25% reduction from 75 mg/m 2 ) Third Dose Reduction* 45 mg/m 2 (20% reduction from 56 mg/m 2 ) Table 2 lists the recommended dosage modifications of FYARRO for adverse reactions. Table 2. Recommended FYARRO Dosage Modifications for Adverse Reactions *Severity based on Common Terminology Criteria for Adverse Events Version 4.03.

Adverse Reaction Severity* Dosage Modifications Stomatitis [see Warnings and Precautions ( 5.1 )] Grade 2 or 3 Withhold FYARRO until Grade ≤1. Restart at the same dose for first occurrence. If recurs, restart at reduced dose level.

Grade 4 Permanently discontinue FYARRO. Anemia [see Warnings and Precautions ( 5.2 )] Grade 2 Withhold FYARRO until Hb ≥8 g/dL. Restart at the same dose level.

Grade ≥3 Withhold FYARRO until Hb ≥8 g/dL. Restart at the same dose level. If recurs, resume at reduced dose level.

Thrombocytopenia [see Warnings and Precautions ( 5.2 )] Grade 2 Withhold FYARRO until platelet count >100×10 9 /L. Restart at the same dose level. Grade ≥3 Withhold FYARRO until platelet count >100×10 9 /L.

Restart at reduced dose level. Neutropenia [see Warnings and Precautions ( 5.2 )] Grade 2 or 3 Withhold FYARRO until absolute neutrophil count ≥1.5×10 9 /L. Restart at the same dose level.

Grade 4 Withhold FYARRO until absolute neutrophil count ≥1.5×10 9 /L. Restart at reduced dose level. Infections [see Warnings and Precautions ( 5.3 )] Grade 3 Withhold FYARRO until resolved.

Restart at reduced dose level. If recurs, permanently discontinue FYARRO. Grade 4 Withhold FYARRO until resolved.

Restart at reduced dose level or permanently discontinue FYARRO. Hypokalemia [see Warnings and Precautions ( 5.4 )] Grade 2 Withhold FYARRO until Grade ≤1. Restart at the same dose level.

If recurs, restart at reduced dose level. Grade ≥3 Withhold FYARRO until Grade ≤1. Restart at reduced dose level.

If recurs, permanently discontinue FYARRO. Hyperglycemia [see Warnings and Precautions ( 5.5 )] Grade ≥3 Withhold FYARRO until Grade ≤2. Restart at reduced dose level.

Interstitial Lung Disease / Non- Infectious Pneumonitis [see Warnings and Precautions ( 5.6 )] Grade 2 Withhold FYARRO for up to 3 weeks until Grade ≤1. Restart at reduced dose level. If not resolved to Grade ≤1 within 3 weeks, permanently discontinue FYARRO.

If recurs, permanently discontinue FYARRO. Grade ≥3 Permanently discontinue FYARRO. Hemorrhage [see Warnings and Precautions ( 5.7 )] Grade 2 or 3 Withhold FYARRO until Grade ≤1.

Resume at reduced dose. If recurs, permanently discontinue FYARRO. Grade 4 Permanently discontinue FYARRO.

Other Adverse Reactions [see Adverse Reactions ( 6.1 )] Grade 3 Withhold FYARRO until Grade ≤1. Restart at the same dose level. If recurs, restart at reduced dose level.

Grade 4 Permanently discontinue FYARRO.

2.3Dosage Modifications for Concomitant Use with CYP3A4 and/or P-gp Inhibitors and Inducers Reduce the dosage of FYARRO to 56 mg/m 2 when used concomitantly with a moderate or weak cytochrome P-450 3A4 (CYP3A4) inhibitor. Avoid concomitant use with drugs that are strong CYP3A4 and/or P-glycoprotein (P-gp) inhibitors and inducers and with grapefruit and grapefruit juice [see Dru… [Excerpted — this section continues on DailyMed.]

💊 Dosage Forms and Strengths 50 words ▾

3 DOSAGE FORMS AND STRENGTHS For injectable suspension: white to yellow, sterile lyophilized powder containing 100 mg of sirolimus formulated as albumin-bound particles in single-dose vial for reconstitution. For injectable suspension: lyophilized powder containing 100 mg of sirolimus formulated as albumin-bound particles in single-dose vial for reconstitution. ( 3 )

⛔ Contraindications 42 words ▾

4 CONTRAINDICATIONS FYARRO is contraindicated in patients with a history of severe hypersensitivity to sirolimus, other rapamycin derivatives, or albumin [see Warnings and Precautions ( 5.8 )] . History of severe hypersensitivity to sirolimus, other rapamycin derivatives, or albumin. ( 4 )

⚠️ Warnings and Cautions ~3 min read ▾

5 WARNINGS AND PRECAUTIONS Stomatitis : Withhold, resume at reduced dose, or permanently discontinue based on severity. ( 5.1 ) Myelosuppression : Monitor blood counts prior to and during FYARRO treatment as clinically indicated. Withhold, resume at reduced dose, or permanently discontinue based on severity.

( 5.2 ) Infections : May result from immunosuppression. Monitor for signs and symptoms of infection. Withhold, resume at reduced dose, or permanently discontinue based on severity.

( 5.3 ) Hypokalemia and hyperglycemia : Monitor serum potassium and glucose prior to starting FYARRO and as clinically indicated. Withhold, resume at reduced dose, or permanently discontinue based on severity. ( 5.4 , 5.5 ) ILD/Non-Infectious Pneumonitis : Monitor for new or worsening respiratory symptoms or radiological changes.

Withhold, resume at reduced dose, or permanently discontinue based on severity. ( 5.6 ) Hemorrhage: Monitor for signs and symptoms. Withhold, resume at reduced dose, or permanently discontinue based on severity.

( 5.7 ) Hypersensitivity Reactions : Monitor for hypersensitivity during and following each FYARRO infusion. Monitor for at least 2 hours following completion of the first infusion and as clinically indicated for each subsequent infusion. Reduce the rate, interrupt infusion, or permanently discontinue based on severity.

( 5.8 ) Embryo-Fetal Toxicity : Can cause fetal harm. Advise patients of the potential hazard to the fetus and to use effective contraception. ( 5.9 ) Male Infertility : Azoospermia or oligospermia may occur.

( 5.10 ) Immunizations : Avoid live vaccines ( 5.11 )

5.1Stomatitis Stomatitis , including mouth ulcers and oral mucositis , occurred in 79% of patients treated with FYARRO, including 18% Grade 3. Stomatitis was most often first reported within 8 weeks of treatment. Based on the severity of the adverse reaction, withhold, resume at reduced dose, or permanently discontinue FYARRO [see Dosage and Administration ( 2.2 ), Adverse Reactions ( 6.1 )] .

5.2Myelosuppression FYARRO can cause myelosuppression including anemia, thrombocytopenia and neutropenia. Anemia occurred in 68% of patients; 6% were Grade 3. Thrombocytopenia and neutropenia occurred in 35% of patients each.

Obtain blood counts at baseline and every 2 months for the first year of treatment and every 3 months thereafter, or more frequently if clinically indicated. Based on the severity of the adverse reaction, withhold, resume at reduced dose, or permanently discontinue FYARRO [see Dosage and Administration ( 2.2 ), Adverse Reactions ( 6.1 )].

5.3Infections FYARRO can cause infections. Infections such as urinary tract infections (UTI), upper respiratory tract infections and sinusitis occurred in 59% of patients. Grade 3 infections occurred in 12% of patients, including a single case each of a UTI, pneumonia, skin, and abdominal infections.

Monitor patients for infections, including opportunistic infections. Based on the severity of the adverse reaction, withhold, resume at reduced dose, or permanently discontinue FYARRO [see Dosage and Administration ( 2.2 ), Adverse Reactions ( 6.1 )] .

5.4Hypokalemia FYARRO can cause hypokalemia. Hypokalemia occurred in 44% of patients, including 12% Grade 3 events. Monitor potassium levels prior to starting FYARRO and implement potassium supplementation as medically indicated. Based on the severity of the adverse reaction, withhold, resume at reduced dose, or permanently discontinue FYARRO [see Dosage and Administration ( 2.2 ), Adverse Reactions ( 6.1 )] .

5.5Hyperglycemia FYARRO can cause hyperglycemia. Hyperglycemia occurred in 12% of patients treated with FYARRO, all of which were Grade 3 events. Monitor fasting serum glucose prior to starting FYARRO.

During treatment, monitor serum glucose every 3 months in non-diabetic patients, or as clinically indicated. Monitor serum glucose more frequently in diabetic patients. Based on the severity of the adverse reaction, withhold, resume at redu… [Excerpted — this section continues on DailyMed.]

🤒 Adverse Reactions ~3 min read ▾

6 ADVERSE REACTIONS The following adverse reactions have been associated with FYARRO in clinical trials and are discussed in greater detail in other sections of the label [see Warnings and Precautions ( 5 )] . Stomatitis [see Warnings and Precautions ( 5.1 )] Myelosuppression [see Warnings and Precautions ( 5.2 )] Infections [see Warnings and Precautions ( 5.3 )] Hypokalemia [see Warnings and Precautions ( 5.4 )] Hyperglycemia [see Warnings and Precautions ( 5.5 )] Interstitial Lung Disease (ILD) / Non-Infectious Pneumonitis [see Warnings and Precautions ( 5.6 )] Hemorrhage [see Warnings and Precautions ( 5.7 )] Hypersensitivity [see Warnings and Precautions ( 5.8 )] The most common (≥30%) adverse reactions were stomatitis, fatigue, rash, infection, nausea, edema, diarrhea, musculoskeletal pain, decreased weight, decreased appetite, cough, vomiting, and dysgeusia.

( 6.1 ) The most common (≥6%) Grade 3 to 4 laboratory abnormalities were decreased lymphocytes, increased glucose, decreased potassium, decreased phosphate, decreased hemoglobin, and increased lipase. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Aadi Bioscience, Inc. at 1-888-BIO-AADI (888-246-2234) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .

6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of FYARRO was assessed in a single-arm study (AMPECT). Thirty-four patients received FYARRO 100 mg/m 2 on Days 1 and 8 of 21-day cycles until disease progression or unacceptable toxicity [see Clinical Studies ( 14.1 )] .

Among the 34 patients who received FYARRO, 16 (47%) were exposed for 6 months or longer and 7 (21%) were exposed for greater than 1 year. The median age of patients who received FYARRO was 59.5 years (range 27 to 78 years), 82% were female and Eastern Cooperative Oncology Group (ECOG) Performance Status was 0 (76%) or 1 (24%). Race was 71% White, 9% Black, 9% Asian, 3% Hawaiian/Pacific Islander and 9% Other/Not Reported.

Ethnicity was 82% not Hispanic or Latino, 15% Hispanic or Latino, and 3% Not Reported. Serious adverse reactions occurred in 14 (41%) patients who received FYARRO. Serious adverse reactions in >5% of patients, including 4 (12%) patients with infection and 2 (6%) patients each with abdominal pain, dehydration, and upper gastrointestinal hemorrhage.

Fatal adverse reactions occurred in 1 (2.9%) patient who received FYARRO and experienced upper gastrointestinal hemorrhage. Permanent discontinuation of FYARRO due to an adverse reaction occurred in 3 (9%) patients. Adverse reactions which resulted in permanent discontinuation of FYARRO included pneumonitis, anemia, and noninfective cystitis.

Dosage interruptions of FYARRO due to an adverse reaction occurred in 22 (65%) patients. Adverse reactions which required dosage interruption in >5% of patients included stomatitis in 6 (18%) patients, pneumonitis in 5 (15%) patients, anemia in 3 (9%) patients, and dehydration, dermatitis acneiform, and thrombocytopenia in 2 (6%) patients each. Dose reductions of FYARRO due to an adverse reaction occurred in 12 (35%) patients.

Adverse reactions which required dose reductions in >5% of patients included stomatitis and pneumonitis in 3 (9%) patients each. The most common adverse reactions (≥30%) were stomatitis in 27 (79%) patients, fatigue and rash in 23 (68%) patients each, infection in 20 (59%) patients, nausea and edema in 17 (50%) patients each, diarrhea, musculoskeletal pain and decreased weight in 16 (47%) patients each, decreased appetite in 15 (44%) patients, cough in 12 (35%) patients, and vomiting and dysgeusia in 11 (32%) patients each.

The most common Grade 3 to 4 laboratory abnormalities (≥6%) were decreased lymphocytes in 7 (21%) patients, increased glucose and decreased potassium in… [Excerpted — this section continues on DailyMed.]

🔄 Drug Interactions 173 words ▾

7 DRUG INTERACTIONS Strong CYP3A4 and/or P-gp Inhibitors or Inducers : Avoid concomitant use. ( 2.3 , 7.1 ) Moderate or Weak CYP3A4 Inhibitors : Reduce FYARRO dose. ( 2.3 , 7.1 )

7.1Effects of Other Drugs on FYARRO CYP3A4 and/or P-gp Inhibitors or Inducers CYP3A4 and/or P-gp inhibitors may increase sirolimus concentrations, which may increase the risk of FYARRO adverse reactions. CYP3A4 and/or P-gp inducers may decrease sirolimus concentrations, which may reduce FYARRO effectiveness. Strong CYP3A4 and/or P-gp Inhibitors or Inducers: Avoid concomitant use of FYARRO with strong CYP3A4 and/or P-gp inhibitors or strong CYP3A4 and/or P-gp inducers [see Dosage and Administration ( 2.3 ), Clinical Pharmacology ( 12.3 )] .

Grapefruit or Grapefruit Juice: Avoid concomitant use of FYARRO with grapefruit or grapefruit juice. Moderate or Weak CYP3A4 Inhibitors: Reduce the dosage of FYARRO when used concomitantly with a moderate or weak CYP3A4 inhibitor [see Dosage and Administration ( 2.3 ), Clinical Pharmacology ( 12.3 )] . Moderate or Weak CYP3A4 Inducers: Use of FYARRO may result in decreased effectiveness.

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS Hepatic Impairment : Reduce the dose of FYARRO in patients with mild or moderate hepatic impairment. Avoid use in patients with severe hepatic impairment. ( 2.4 , 8.6 ) Lactation : Advise not to breastfeed. ( 8.2 ) Females and Males of Reproductive Potentia l: May impair fertility in females and males. ( 5.9 , 5.10 , 8.3 )

8.1Pregnancy Risk Summary Based on animal studies and the mechanism of action, FYARRO can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )] . Although there are no data on the use of FYARRO in pregnant women, there are limited data on the use of sirolimus during pregnancy. In animal studies, oral sirolimus was embryo/fetotoxic in rats [see Data ] at sub-therapeutic doses.

Advise pregnant women of the potential risk to a fetus. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively.

Data Animal Data Reproductive studies in animals have not been performed with FYARRO. Studies with an oral formulation of sirolimus have shown that it crosses the placenta and is toxic to the conceptus. In rat embryo-fetal development studies, pregnant rats were administered an oral formulation of sirolimus during the period of organogenesis (Gestational Day 6-15).

Sirolimus produced embryo-fetal lethality at 0.5 mg/kg and reduced fetal weight at 1 mg/kg. The no observed adverse effect level (NOAEL) for fetal toxicity in rats was 0.1 mg/kg. Maternal toxicity (weight loss) was observed at 2 mg/kg.

The NOAEL for maternal toxicity was 1 mg/kg. In rabbit embryo-fetal development studies, pregnant rabbits were administered an oral formulation of sirolimus during the period of organogenesis (Gestational Day 6-18). There were no effects on embryo-fetal development at doses up to 0.05 mg/kg; however, at doses of 0.05 mg/kg and above, the ability to sustain a pregnancy was impaired (i.e., embryo-fetal abortion or early resorption).

Maternal toxicity (decreased body weight) was observed at 0.05 mg/kg. The NOAEL for maternal toxicity was 0.025 mg/kg. In a pre- and post-natal development study in rats, pregnant females were dosed with an oral formation of sirolimus during gestation and lactation (Gestational Day 6 through Lactation Day 20).

An increased incidence of dead pups occurred at 0.5 mg/kg, resulting in reduced live litter size. At 0.1 mg/kg, there were no adverse effects on offspring. Sirolimus did not cause maternal toxicity or affect developmental parameters in the surviving offspring (e.g., morphological development, motor activity, learning, or fertility assessment) at 0.5 mg/kg, the highest oral dose tested.

8.2Lactation Risk Summary There are no data on the presence of FYARRO in human milk or its effects on the breastfed child or on milk production. It is not known whether sirolimus is present in human milk. There are no data on its effects on the breastfed infant or milk production.

The pharmacokinetic and safety profiles of sirolimus in infants are not known. Sirolimus is present in the milk of lactating rats. There is potential for serious adverse effects from sirolimus in breastfed infants based on mechanism of action [see Clinical Pharmacology ( 12.1 )] .

Because of the potential for serious adverse reactions in breastfed infants from FYARRO, advise women not to breastfeed during treatment with FYARRO and for 2 weeks after the last dose.

8.3Females and Males of Reproductive Potential FYARRO can cause fetal harm when administered to a pregnant woman [see Warnings and Precautions ( 5.9 ), Use in Specific Populations ( 8.1 )]. Pregnancy Testing Verify pregnancy status of females of reproductive potential prior to initiating FYARRO. Contraception Females Advise females of reproductive potential to use effective contraception during… [Excerpted — this section continues on DailyMed.]

🤰 Pregnancy ~2 min read ▾

8.1Pregnancy Risk Summary Based on animal studies and the mechanism of action, FYARRO can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )] . Although there are no data on the use of FYARRO in pregnant women, there are limited data on the use of sirolimus during pregnancy. In animal studies, oral sirolimus was embryo/fetotoxic in rats [see Data ] at sub-therapeutic doses.

Advise pregnant women of the potential risk to a fetus. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively.

Data Animal Data Reproductive studies in animals have not been performed with FYARRO. Studies with an oral formulation of sirolimus have shown that it crosses the placenta and is toxic to the conceptus. In rat embryo-fetal development studies, pregnant rats were administered an oral formulation of sirolimus during the period of organogenesis (Gestational Day 6-15).

Sirolimus produced embryo-fetal lethality at 0.5 mg/kg and reduced fetal weight at 1 mg/kg. The no observed adverse effect level (NOAEL) for fetal toxicity in rats was 0.1 mg/kg. Maternal toxicity (weight loss) was observed at 2 mg/kg.

The NOAEL for maternal toxicity was 1 mg/kg. In rabbit embryo-fetal development studies, pregnant rabbits were administered an oral formulation of sirolimus during the period of organogenesis (Gestational Day 6-18). There were no effects on embryo-fetal development at doses up to 0.05 mg/kg; however, at doses of 0.05 mg/kg and above, the ability to sustain a pregnancy was impaired (i.e., embryo-fetal abortion or early resorption).

Maternal toxicity (decreased body weight) was observed at 0.05 mg/kg. The NOAEL for maternal toxicity was 0.025 mg/kg. In a pre- and post-natal development study in rats, pregnant females were dosed with an oral formation of sirolimus during gestation and lactation (Gestational Day 6 through Lactation Day 20).

An increased incidence of dead pups occurred at 0.5 mg/kg, resulting in reduced live litter size. At 0.1 mg/kg, there were no adverse effects on offspring. Sirolimus did not cause maternal toxicity or affect developmental parameters in the surviving offspring (e.g., morphological development, motor activity, learning, or fertility assessment) at 0.5 mg/kg, the highest oral dose tested.

🧒 Pediatric Use 16 words ▾

8.4Pediatric Use The safety and efficacy of FYARRO in pediatric patients have not been established.

🧓 Geriatric Use 51 words ▾

8.5Geriatric Use Of the 34 patients treated with FYARRO, 44% were 65 years of age and older, and 6% were 75 years of age and older. Clinical studies of FYARRO did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently from younger patients.

🧬 Clinical Pharmacology ~2 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action Sirolimus in FYARRO is an inhibitor of mechanistic target of rapamycin kinase (mTOR, previously known as mammalian target of rapamycin). mTOR, a serine threonine kinase, is downstream of the PI3K/AKT pathway, controls key cellular processes such as cell survival, growth, and proliferation, and is commonly dysregulated in several human cancers. In cells, sirolimus binds to the immunophilin, FK Binding Protein-12 (FKBP-12), to generate an immunosuppressive complex. The sirolimus-FKBP-12 complex binds to and inhibits activation of the mechanistic target of rapamycin complex 1 (mTORC1).

Inhibition of mTOR by sirolimus has been shown to reduce cell proliferation, angiogenesis, and glucose uptake in in vitro and in vivo studies. In a nonclinical study in athymic mice bearing human tumor xenografts, intravenous administration of FYARRO resulted in higher tumor accumulation of sirolimus, inhibition of an mTOR target in the tumor, and tumor growth inhibition compared to administration of an oral formulation of sirolimus at the same weekly total dose.

12.2Pharmacodynamics Sirolimus exposure-response relationship has not been fully characterized. Cardiac Electrophysiology The effect of FYARRO on the QTc interval has not been adequately characterized.

12.3Pharmacokinetics Absorption Following administration of FYARRO at the recommended dosage, the estimated mean (%CV) C max and AUC 0-inf of sirolimus in patients with advanced solid tumors were 2590 ng/mL (30% CV) and 22100 ng∙h/mL (50% CV), respectively. Distribution The protein binding of sirolimus is >99%, primarily to serum albumin in vitro . Elimination The mean elimination half-life of sirolimus is approximately 59 hours (41% CV).

Metabolism Sirolimus is metabolized by CYP3A4. Excretion Following a single radiolabeled sirolimus oral dose to human subjects, 91% and 2% of the radioactivity was recovered in feces and urine, respectively. Specific Populations There were no clinically significant differences in the pharmacokinetics of sirolimus based on age (18 to 78 years), sex, mild or moderate renal impairment (creatinine clearance 30 to 89 mL/min).

The effect of race, severe renal impairment, and hepatic impairment on the pharmacokinetics of sirolimus is unknown. Drug Interaction Studies No studies evaluating the drug interaction potential of FYARRO have been conducted. Sirolimus is a substrate for both CYP3A4 and P-gp.

🧬 Mechanism of Action 159 words ▾

12.1Mechanism of Action Sirolimus in FYARRO is an inhibitor of mechanistic target of rapamycin kinase (mTOR, previously known as mammalian target of rapamycin). mTOR, a serine threonine kinase, is downstream of the PI3K/AKT pathway, controls key cellular processes such as cell survival, growth, and proliferation, and is commonly dysregulated in several human cancers. In cells, sirolimus binds to the immunophilin, FK Binding Protein-12 (FKBP-12), to generate an immunosuppressive complex. The sirolimus-FKBP-12 complex binds to and inhibits activation of the mechanistic target of rapamycin complex 1 (mTORC1).

Inhibition of mTOR by sirolimus has been shown to reduce cell proliferation, angiogenesis, and glucose uptake in in vitro and in vivo studies. In a nonclinical study in athymic mice bearing human tumor xenografts, intravenous administration of FYARRO resulted in higher tumor accumulation of sirolimus, inhibition of an mTOR target in the tumor, and tumor growth inhibition compared to administration of an oral formulation of sirolimus at the same weekly total dose.

📦 How Supplied / Storage and Handling 77 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING FYARRO (sirolimus protein-bound particles for injectable suspension) (albumin-bound) is a white to yellow, sterile lyophilized powder supplied as: NDC 80803-153-50, 100 mg of sirolimus in a single-dose vial. Each carton contains 1 vial. Store the vials in the original cartons at 2° to 8°C [USP Refrigerated Temperature] (36° to 46°F).

Retain in the original package to protect from light. FYARRO is a hazardous drug. Follow applicable special handling and disposal procedures.

1

📋 Description 181 words ▾

11 DESCRIPTION FYARRO (sirolimus protein-bound particles for injectable suspension) (albumin-bound) is sirolimus formulated as albumin-bound nanoparticles. The active ingredient in FYARRO is sirolimus bound to albumin which exists in the nanoparticles in a non-crystalline, amorphous state. Sirolimus is a mechanistic target of rapamycin kinase (mTOR) inhibitor.

Sirolimus is a macrocyclic lactone produced by Streptomyces hygroscopicus . The chemical name of sirolimus is [3S[3R*[S*(1R*,3S*,4S*)),6S*,7E,9S*,10S*,12S*,14R*,15E,17E,19E,21R*,23R*,26S*, 27S*,3 4aR*]]-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-Hexadecahydro-9,27-dihydroxy 3-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylethyl]-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-23,27-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone. Its empirical formula is C 51 H 79 NO 13 , and the molecular weight is 914.2.

The structural formula of sirolimus is illustrated as follows: Sirolimus is a white to off-white crystalline powder and is insoluble in water but freely soluble in benzyl alcohol, chloroform, acetone, and acetonitrile. FYARRO is supplied as a white to yellow, sterile, lyophilized powder for reconstitution with 20 mL of 0.9% Sodium Chloride Injection, USP prior to intravenous infusion. Each single-dose vial contains 100 mg of sirolimus (bound to human albumin) and approximately 850 mg of human albumin (containing sodium caprylate and sodium acetyltryptophanate).

Each milliliter (mL) of reconstituted suspension contains 5 mg sirolimus formulated as albumin-bound particles. Figure

💬 Information for Patients ~2 min read ▾

17 PATIENT COUNSELING INFORMATION Stomatitis Advise patients of the risk of stomatitis [see Warnings and Precautions ( 5.1 )] . Myelosuppression Advise patients of the risk of myelosuppression and the need to monitor blood counts periodically during therapy [see Warnings and Precautions ( 5.2 )]. Infections Advise patients that they are more susceptible to infections and that they should immediately report any signs or symptoms of infection to their healthcare provider [see Warnings and Precautions ( 5.3 )] .

Hypokalemia Advise patients of the risk of hypokalemia and the need to monitor potassium periodically during therapy [see Warnings and Precautions ( 5.4 )] . Hyperglycemia Advise patients of the risk of hyperglycemia and the need to monitor glucose periodically during therapy [see Warnings and Precautions ( 5.5 )] . Interstitial Lung Disease / Non-Infectious Pneumonitis Advise patients of the risk of developing non-infectious pneumonitis and to immediately report any new or worsening respiratory symptoms to their healthcare provider [see Warnings and Precautions ( 5.6 )] .

Hemorrhage Advise patients of the risk of hemorrhage. Instruct patients to report signs of bleeding, and to seek immediate medical attention for signs or symptoms of severe bleeding [see Warnings and Precautions ( 5.7 )]. Hypersensitivity Reactions Advise patients of the risk of clinically significant hypersensitivity reactions and to promptly contact their healthcare provider or seek emergency care for signs of hypersensitivity reaction including rash, itching, hives, difficulty breathing or swallowing, flushing, chest pain, or dizziness [see Contraindications ( 4 ), Warnings and Precautions ( 5.8 )] .

Embryo-Fetal Toxicity Advise females of reproductive potential of the potential risk to a fetus and to inform their healthcare provider of a known or suspected pregnancy [see Warnings and Precautions ( 5.9 )]. Advise females of reproductive potential to use effective contraception during treatment and for 12 weeks after the last dose [see Use in Specific Populations ( 8.1 , 8.3 )]. Advise males with female partners of reproductive potential to use effective contraception during treatment and for 12 weeks after the last dose [see Warnings and Precautions ( 5.9 ), Use in Specific Populations ( 8.3 )] .

Infertility Advise males and females of reproductive potential of the potential risk for impaired fertility [see Warnings and Precautions ( 5.10 ), Use in Specific Populations ( 8.3 )] . Immunizations Advise patients that vaccinations may be less effective while being treated with FYARRO. Advise patients to avoid the use of live vaccines, and close contact with those who have received live vaccines, while on FYARRO [see Warnings and Precautions ( 5.11 )] .

Lactation Advise women not to breastfeed during treatment with FYARRO and for 2 weeks after the last dose [see Use in Specific Populations ( 8.2 )] . Drug Interactions Advise patients to inform their healthcare provider about all concomitant medications, including prescription medicine, over the counter drugs, vitamins, and herbal products [see Drug Interactions ( 7 )]. Inform patients to avoid grapefruit and grapefruit juice while taking FYARRO.

This product's label may have been updated. For current full prescribing information, please visit www.aadibio.com . Manufactured for Aadi Bioscience, Inc., Morristown, NJ 07960.

FYARRO ® is a registered trademark of Aadi Bioscience, Inc. Patent: www.aadibio.com/patents/

🧬 Pharmacokinetics 170 words ▾

12.3Pharmacokinetics Absorption Following administration of FYARRO at the recommended dosage, the estimated mean (%CV) C max and AUC 0-inf of sirolimus in patients with advanced solid tumors were 2590 ng/mL (30% CV) and 22100 ng∙h/mL (50% CV), respectively. Distribution The protein binding of sirolimus is >99%, primarily to serum albumin in vitro . Elimination The mean elimination half-life of sirolimus is approximately 59 hours (41% CV).

Metabolism Sirolimus is metabolized by CYP3A4. Excretion Following a single radiolabeled sirolimus oral dose to human subjects, 91% and 2% of the radioactivity was recovered in feces and urine, respectively. Specific Populations There were no clinically significant differences in the pharmacokinetics of sirolimus based on age (18 to 78 years), sex, mild or moderate renal impairment (creatinine clearance 30 to 89 mL/min).

The effect of race, severe renal impairment, and hepatic impairment on the pharmacokinetics of sirolimus is unknown. Drug Interaction Studies No studies evaluating the drug interaction potential of FYARRO have been conducted. Sirolimus is a substrate for both CYP3A4 and P-gp.

🧬 Pharmacodynamics 25 words ▾

12.2Pharmacodynamics Sirolimus exposure-response relationship has not been fully characterized. Cardiac Electrophysiology The effect of FYARRO on the QTc interval has not been adequately characterized.

🔬 Clinical Studies ~1 min read ▾

14 CLINICAL STUDIES

14.1Perivascular Epithelioid Cell Tumor (PEComa) The efficacy of FYARRO was assessed in AMPECT (NCT02494570), a multi-center, single-arm clinical trial in 31 patients with locally advanced unresectable or metastatic malignant PEComa. Patients were required to have measurable disease at baseline, centrally confirmed diagnosis by pathology of malignant PEComa, and Eastern Cooperative Oncology Group (ECOG) Performance Status (PS) of 0 or 1. Patients with lymphangioleiomyomatosis and prior treatment with a mTOR inhibitor were excluded.

Patients received FYARRO at a dose of 100 mg/m 2 on Days 1 and 8 of 21-day cycles until disease progression or unacceptable toxicity. The efficacy population of 31 patients had the following demographic characteristics: median age 60 years (range 34 to 78), 81% female, 74% White, 10% Black, and 81% ECOG PS of 0. Five (16%) patients had locally advanced disease and 26 (84%) had metastatic disease.

Ninety-four percent of patients had prior surgery,19% had prior radiation therapy, and 13% had prior systemic therapy. The major efficacy outcome measures were overall response rate (ORR) and duration of response (DOR) as assessed by blinded independent central review (BICR) using RECIST v.1.1. The efficacy results are summarized in Table 6 .

Table 6. Efficacy Results in AMPECT * All responses were initially partial responses. Two patients with partial response converted to complete response during the follow up-period. + Denotes ongoing responses CI = Confidence Interval; NR = Not Reached; NE = Not Estimable Efficacy Endpoints FYARRO (N=31) Overall Response Rate (95% CI)* 39% (22%, 58%) Duration of Response (DOR) (N=12) Median (95% CI) in months NR (6.5, NE) Range in months 5.6, 55.5+ % with duration ≥6 months 92% % with duration ≥12 months 67% % with duration ≥24 months 58%

🧪 Nonclinical Toxicology ~1 min read ▾

13 NONCLINICAL TOXICOLOGY

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility No carcinogenicity, mutagenesis, or fertility studies were conducted with FYARRO. Carcinogenicity studies have been conducted in mice and rats with an oral formulation of sirolimus. In an 86-week female mouse study, there was a statistically significant increase in malignant lymphoma at all dose levels compared with controls.

In a second mouse study, hepatocellular adenoma and carcinoma in males were considered sirolimus-related. In a 104-week rat study, there were no significant findings. Sirolimus was not genotoxic in an in vitro bacterial reverse mutation assay, a Chinese hamster ovary cell chromosomal aberration assay, a mouse lymphoma cell forward mutation assay, or an in vivo mouse micronucleus assay.

When female rats were treated by gavage with an oral formulation of sirolimus and mated to untreated males, female fertility was decreased at 0.5 mg/kg due to decreased implantation. In addition, reduced ovary and uterus weight were observed. The NOAEL for female rat fertility was 0.1 mg/kg.

When male rats were treated by gavage with an oral formulation of sirolimus and mated to untreated females, male fertility was decreased at 2 mg/kg. Atrophy of testes, epididymides, prostate, seminiferous tubules, and reduced sperm counts were observed. The NOAEL for male rat fertility was 0.5 mg/kg.

Testicular tubular degeneration was also seen in a 4-week intravenous study of sirolimus in monkeys at 0.1 mg/kg.

📄 Carcinogenesis, Mutagenesis, Impairment of Fertility ~1 min read ▾

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility No carcinogenicity, mutagenesis, or fertility studies were conducted with FYARRO. Carcinogenicity studies have been conducted in mice and rats with an oral formulation of sirolimus. In an 86-week female mouse study, there was a statistically significant increase in malignant lymphoma at all dose levels compared with controls.

In a second mouse study, hepatocellular adenoma and carcinoma in males were considered sirolimus-related. In a 104-week rat study, there were no significant findings. Sirolimus was not genotoxic in an in vitro bacterial reverse mutation assay, a Chinese hamster ovary cell chromosomal aberration assay, a mouse lymphoma cell forward mutation assay, or an in vivo mouse micronucleus assay.

When female rats were treated by gavage with an oral formulation of sirolimus and mated to untreated males, female fertility was decreased at 0.5 mg/kg due to decreased implantation. In addition, reduced ovary and uterus weight were observed. The NOAEL for female rat fertility was 0.1 mg/kg.

When male rats were treated by gavage with an oral formulation of sirolimus and mated to untreated females, male fertility was decreased at 2 mg/kg. Atrophy of testes, epididymides, prostate, seminiferous tubules, and reduced sperm counts were observed. The NOAEL for male rat fertility was 0.5 mg/kg.

Testicular tubular degeneration was also seen in a 4-week intravenous study of sirolimus in monkeys at 0.1 mg/kg.

📚 References 7 words ▾

15 REFERENCES OSHA Hazardous Drugs. OSHA. https://www.osha.gov/SLTC/hazardousdrugs/index.html.

📄 Package Label / Principal Display Panel 34 words ▾

PRINCIPAL DISPLAY PANEL NDC 80803-153-50 Rx Only Fyarro ™ sirolimus protein-bound particles for injectable suspension (albumin-bound) 100 mg per vial For intravenous infusion Single-dose vial Discard any unused portion. Principal display panel - Carton

Source: FDA Structured Product Labeling, mirrored from DailyMed / openFDA. Prefer the government’s original formatting? View this label on DailyMed ↗

Medicaid utilization & spend

📍 This exact package only: Medicaid data is reported per full 11-digit NDC — labeler, product and pack size — so every number here is for this package alone, not the drug overall. Other pack sizes report separately.
💊 Pharmacy benefit only: These are Medicaid outpatient pharmacy claims, billed by NDC. They exclude the medical benefit — clinic- or hospital-administered drugs billed under HCPCS J-codes — so drugs used mostly that way (e.g. Avastin, Lucentis, Keytruda) can look low or missing here. That’s expected, not an error.
📅 Q1 2025 – Q1 2026 · 5 quarters of data
ⓘ The newest quarter is usually incomplete when first published; states restate recent quarters in later CMS releases, so the latest figures typically revise upward. State coverage-policy changes can also shift quarter-to-quarter totals.
Prescriptions last 4 qtrs
146
Units reimbursed last 4 qtrs
144
Gross reimbursed last 4 qtrs
$914.4K
Avg / prescription
$6,263.12
Avg / unit
$6,328.57
Latest quarter Q1 2026
25Rx
Fee-for-service vs managed care ⓘ
20% FFS 80% MCO
Fee-for-service · 29 Rx Managed care · 117 Rx
State Medicaid map
Alaska: no data reported AK Maine: no data reported ME Washington: no data reported WA Idaho: no data reported ID Montana: no data reported MT North Dakota: no data reported ND Minnesota: no data reported MN Wisconsin: no data reported WI Michigan: 29 units · 0.3 per 100k residents MI New York: no data reported NY Vermont: no data reported VT New Hampshire: 49 units · 3.5 per 100k residents NH Oregon: no data reported OR Nevada: no data reported NV Wyoming: no data reported WY South Dakota: no data reported SD Iowa: no data reported IA Illinois: no data reported IL Indiana: no data reported IN Ohio: no data reported OH Pennsylvania: no data reported PA New Jersey: no data reported NJ Massachusetts: no data reported MA California: no data reported CA Utah: no data reported UT Colorado: no data reported CO Nebraska: no data reported NE Missouri: no data reported MO Kentucky: no data reported KY West Virginia: no data reported WV Virginia: no data reported VA Maryland: no data reported MD Connecticut: no data reported CT Rhode Island: no data reported RI Arizona: no data reported AZ New Mexico: no data reported NM Kansas: 26 units · 0.9 per 100k residents KS Arkansas: no data reported AR Tennessee: no data reported TN North Carolina: no data reported NC South Carolina: no data reported SC Delaware: 40 units · 3.9 per 100k residents DE Oklahoma: no data reported OK Louisiana: no data reported LA Mississippi: no data reported MS Alabama: no data reported AL Georgia: no data reported GA D.C.: no data reported DC Hawaii: no data reported HI Texas: no data reported TX Florida: no data reported FL
Units reimbursed · per 100k residents
0.33.9
gray = no data reported ⓘ
Colors are per 100,000 residents, so big states don’t automatically dominate. Tap or hover a state for its actual totals.
Tap or hover a state
…for its Medicaid breakdown
🏆 Top states by units · per 100k residents
1 Delaware 3.9 /100k
2 New Hampshire 3.5 /100k
3 Kansas 0.9 /100k
4 Michigan 0.3 /100k
National units — by quarter
💵 About the dollar figures: “reimbursed” is what Medicaid paid pharmacies before confidential manufacturer rebates, so the program’s real net cost is lower than these numbers. Fee-for-service and managed-care claims are combined unless split above. Source: CMS State Drug Utilization Data; per-100k rates use 2023 Census population estimates.

Medicare Part D spend CMS · PART D · 2026 (Q1)

Medicare Part D (outpatient prescription) spending for Sirolimus (matched by generic name) — the program that covers self-administered drugs. 11 manufacturers.
⚠️ Drug-level data: CMS publishes Part D spending by drug, not by NDC — these figures combine every manufacturer, strength and package size sold under the name Sirolimus. CMS lists 2 products for this generic; we show the highest-spend one. That’s a different level of aggregation than the Medicaid card above, which is specific to this exact 11-digit NDC (pack size included), so the two aren’t directly comparable.
Period
Total Part D spend
$3.98M
Claims incl. refills
12.6K
Beneficiaries
6.3K
Spend / beneficiary
$630.81
Spend / claim
$314.93
Trend by period
💵 About the dollar figures: spending is what Part D plans paid before confidential manufacturer rebates, so the program’s real net cost is lower. A blank patient count means fewer than 11 people — CMS hides counts that small to protect privacy. Source: CMS Medicare Quarterly Part D Spending by Drug (data.cms.gov), updated quarterly.

Reported adverse events (FAERS)

Read carefully: FAERS reports are voluntary and unverified. Counts are not incidence, do not establish causation, are subject to reporting bias, and cannot be used to compare one drug to another. Shown for signal context only. Reports for Sirolimus — the ingredient across all brands.

Top reported reactions

Pyrexia524
Diarrhoea514
Pneumonia487
Drug Interaction448
Acute Kidney Injury434
Thrombotic Microangiopathy376
Transplant Rejection372

Age at onset

Neonate67
Infant167
Child317
Adolescent188
Adult1,255
Elderly308

Reporter sex

13,367 reports
Male · 57%
Female · 43%
Unknown · 0%

Serious outcomes

Hospitalization4,559
Death2,150
Life-threatening976
Disabling94
Reports over time (by year) — tap or hover for the count & year
2019 2021 2023 2026 1,583 705
Most recent year is provisional (FAERS lags ~3 months).
Where does this data come from?
Adverse-event reports from the FDA Adverse Event Reporting System (FAERS) via openFDA. FAERS reports are voluntary and unverified — counts are not incidence and don’t establish causation.

About this NDC listing & data coverage

Finished prescription product
What data is (and isn’t) available for this NDC — tap to expand
NDC identity (package / product / labeler codes) ✓ Available
Labeler ✓ Available
Product & package description ✓ Available
Marketing category & status ✓ Available
Active ingredient / dosage form / route ✓ Available
FDA label (SPL via DailyMed) ✓ Available
Package photos ✓ Available
Inactive ingredients (structured) ✓ Available
NADAC pharmacy acquisition price (CMS) — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey.
Orange Book / therapeutic-equivalence data ✓ Available
HCPCS J-code billing crosswalk ✓ Available
Medicaid utilization (CMS SDUD) ✓ Available
“Not published” reflects what the public FDA / CMS / NLM sources provide for this exact package code — it is a property of the data feeds, not a judgment about the product.

Questions about this listing

Why is there no price listed?
The pricing shown on our NDC pages comes from CMS NADAC, a voluntary survey of retail community pharmacy invoices. CMS does not publish a NADAC for every NDC — packages outside the retail survey (institutional and hospital products, bulk packages, discontinued items, and many OTC items) may never receive one. A missing price reflects the survey's scope, not this product's actual cost, and does not mean the product is free or unavailable.
Is the NDC printed on the package the same as the 11-digit billing NDC?
Yes, they identify this exact package in different formats. The form printed on the packaging and shown on DailyMed is the one the FDA registered. Insurance claims use a fixed 11-digit 5-4-2 format, so the short segment is padded with a leading zero and the dashes are dropped. The Identity section at the top of this page lists each form of this code.
Is this package still being marketed?
Yes, per the latest FDA NDC Directory data on this page: this package is listed as actively marketed, with no marketing end date reported by Aadi Bioscience, Inc.. Listing status can change — the directory data on this page refreshes weekly.
Who lists this product with the FDA?
Aadi Bioscience, Inc. is the labeler of record for this NDC — the company under whose FDA-assigned code the package is listed. The labeler may be the manufacturer itself or a distributor marketing the product under its own code.
Do I need a prescription for this product?
This NDC is listed with FDA as a prescription product, so it is dispensed under a prescriber's order. Your pharmacist can tell you whether any over-the-counter forms of the same medication exist.
Does this product have a billing J-code?
Yes — this NDC cross-references HCPCS code J9331 for medical-claim billing (typically used when a product is administered in a clinical setting rather than dispensed at a retail pharmacy). See the Billing section on this page.
This page identifies an FDA-listed package (the NDC) and reports public regulatory and pricing data about the listing. It is reference information, not a medical recommendation — talk to your pharmacist or prescriber about your own medication.
Where does this data come from?
Listing facts (marketing category, packager status, marketing dates) from the FDA openFDA NDC Directory; label availability from DailyMed; pricing coverage from CMS NADAC; equivalence scope from the FDA Orange Book.
For educational and professional reference only — not medical advice. Pricing reflects published NADAC and CMS ASP (free public data) and may differ from your acquisition cost; always verify before billing or dispensing.