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Orladeyo Berotralstat hydrochloride 96 mg Pellet — NDC 72769-0112-02 package photo

Orladeyo Berotralstat hydrochloride 96 mg Pellet

by BioCryst Pharmaceuticals, Inc. · 4 DOSE PACK in 1 CARTON (72769-112-02) / 7 PACKET in 1 DOSE PACK / 16 PELLET in 1 PACKET
NDC 72769-0112-02
🏷️ FDA NDC (as labeled) 72769-112-02 billing pads the product segment with a zero
Rx only Brand On market Non-controlled
🗂️ Data synced Sep 3, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →

This page is curated, coded, and maintained by

Compiled from public FDA, CMS, DailyMed, NADAC, and related drug data sources. Editorial policy

🆔 Identity & classification

FDA NDC (as labeled) 72769-112-02
Product NDC 72769-112
11-digit billing NDC 72769011202
NCPDP billing unit EA — each (per item)
RxCUI 2467565, 2467571, 2467573, 2467575, 2728874, 2728878, 2728880, 2728882,
UNII 88SH1NBL2B
Application # NDA219776
SPL Set ID 3527ece1-e7e0-40b1-b0c5-6baeb0deabeb
Established class (EPC) Plasma Kallikrein Inhibitor
Mechanism of action Cytochrome P450 2D6 Inhibitors; Cytochrome P450 3A4 Inhibitors; Kallikrein Inhibitors; P-Glycoprotein Inhibitors
DEA schedule Non-controlled
Marketing category NDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2025-12-12
Route ORAL
Dosage form PELLET
Substance BEROTRALSTAT HYDROCHLORIDE
GCN Seq No 088684
GCN 58833
HICL code 047016
Ingredient (HICL) Berotralstat Hydrochloride
HIC1 code A
Therapeutic class — broad (HIC1) Cardiovascular System
HIC2 code A7
Therapeutic class — intermediate (HIC2) Vasoactive Drugs
HIC3 code A7N
Therapeutic class — specific (HIC3) Plasma Kallikrein Inhibitors
AHFS code 24:48.08.00
AHFS class Kallikrein Inhibitors (24:48:08)
FDB label name ORLADEYO 96 MG PELLET PACKET
FDB brand name Orladeyo
Legend status F — Federal legend — prescription drug or device
Why two NDCs? The FDA registers this code as 72769-112-02 — 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 → 72769-0112-02. 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.

🏷️ RxNorm drug class

This medicine belongs to the Plasma Kallikrein Inhibitor class.

Pharmacologic class Plasma Kallikrein Inhibitor
Drug family (ATC) Drugs used in hereditary angioedema
How it works Cytochrome P450 2D6 Inhibitors, Cytochrome P450 3A4 Inhibitors, Kallikrein Inhibitors, P-Glycoprotein Inhibitors
Where does this data come from?
Therapeutic classes from RxNorm RxClass (U.S. National Library of Medicine) — Established Pharmacologic Class (FDA), ATC drug family (WHO) and mechanism of action, matched by this product’s RxCUI.

🏭 Manufacturer & labeler

LabelerBioCryst Pharmaceuticals, Inc.
Application holderBIOCRYST PHARMACEUTICALS INC
FDA applicationNDA219776 (NDA)
Labeler code72769
First marketedDec 2025
Product typeHuman Prescription Drug
Portfolio7 products on file
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.

🩺 Clinical

Label name ORLADEYO 96 MG PELLET PACKET Ingredient Berotralstat Hydrochloride
📖 What it is MedlinePlus · NLM

Berotralstat is used to prevent attacks of hereditary angioedema (HAE; genetic condition that causes repeat episodes of swelling). Berotralstat is in a class of medications called plasma kallikrein inhibitors. It works by blocking a substance in the body that causes symptoms of angioedema.

Read the full MedlinePlus article ↗
📗 Our plain-language guide HelloPharmacist
  • Orladeyo is a preventive medication — it works in the background every day to reduce how often your HAE attacks happen. It blocks an enzyme in your blood called plasma kallikrein,...
  • What exactly is Orladeyo supposed to do for me?
  • No — Orladeyo is not designed or approved to treat an active attack. Taking extra doses to try to stop a flare won't help, and it's actually unsafe because higher doses can affect...
  • Can I take Orladeyo to stop an HAE attack that's happening right now?
📖 Read our full Berotralstat 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.

💊 What it looks like

Color White / Blue
ShapeCapsule
Imprint110;BCX
Size18 mm
ScoringNot scored
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 2S7830E561
    Crospovidone is a synthetic polymer derived from povidone. It acts as a disintegrant, helping the tablet or capsule break apart quickly in the stomach so the active ingredient can be absorbed.
  • UNII 905HNO1SIH
    A synthetic polymer made from methacrylate compounds that forms a film coating on tablets or capsules. It helps control how quickly the medicine dissolves and releases its active ingredient in the digestive system.
  • UNII 70097M6I30
    Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
  • UNII ETJ7Z6XBU4
    Silicon dioxide is a naturally occurring mineral used as a glidant and anti-caking agent. It helps powder ingredients flow smoothly and prevents clumping during manufacturing and storage.
  • UNII 368GB5141J
    A detergent and foaming agent derived from coconut or palm oil. In medications, it helps break down and mix oil and water-based ingredients, aids in tablet disintegration, and improves how the drug dissolves and spreads in the mouth or digestive system.
  • UNII O8232NY3SJ
    A plant-based carbohydrate derived from corn kernels. It acts as a filler to add bulk, a binder to hold ingredients together, and a disintegrant to help the tablet break apart in your stomach for absorption.
  • UNII 4ELV7Z65AP
    Stearic acid is a fatty acid derived from plant or animal sources. It acts as a binder and lubricant in tablets and capsules, helping them hold together and flow smoothly during manufacturing.
  • UNII 7SEV7J4R1U
    A powder made from a naturally occurring mineral. In medicines, talc works as a glidant and anti-caking agent, helping tablets and capsules flow smoothly during manufacturing and preventing clumping.
  • UNII 15FIX9V2JP
    Titanium dioxide is a bright white mineral powder commonly used as a colorant and opacifying agent. It makes pills and tablets white or lighter in color and helps make coatings non-transparent.

9 inactive ingredients 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.

💲 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 eachPer package
Retail pharmacies payNADAC · weekly Not in the retail survey — common for institutional, discontinued, or low-volume packs.
Medicaid paysCMS SDUD · 12 mo No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data.
Medicare drug plans payPart D · Q2 2026 $1,722.83 $771,828.83 / 448 pellets
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.

🔁 Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Orladeyo 96 mgthis 72769-0112-02 BioCryst 4 doses — — 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

🏛️
2025
First FDA approval
Dec 2025
📍
2026
Currently FDA-listed
1 year 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 May 2040. This may affect when a full generic version becomes widely available, but it is not a guaranteed launch date.
📅 FDA approved Dec 11, 2025 RLD RS ⏳ ~13.6 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 12344585 — method of use (U-4535)
US 12344585 — method of use (U-4535)
US 12344585 — method of use (U-4535)
US 12344585 — method of use (U-4535)
US 11708333 — method of use (U-4535)
US 11708333 — method of use (U-4535)
US 11708333 — method of use (U-4535)
US 11708333 — method of use (U-4535)
US 11618733 — method of use (U-4535)
US 11618733 — method of use (U-4535)
US 11618733 — method of use (U-4535)
US 11618733 — method of use (U-4535)
US 11117867 — method of use (U-4535)
US 11117867 — method of use (U-4535)
US 11117867 — method of use (U-4535)
US 11117867 — method of use (U-4535)
US 11230530 — method of use (U-4535)
US 11230530 — method of use (U-4535)
US 11230530 — method of use (U-4535)
US 11230530 — method of use (U-4535)
US 10125102 — drug substance (U-4535)
US 10125102 — drug substance (U-4535)
US 10125102 — drug substance (U-4535)
US 10125102 — drug substance (U-4535)
US 10662160 — drug substance (U-4535)
US 10662160 — drug substance (U-4535)
US 10662160 — drug substance (U-4535)
US 10662160 — drug substance (U-4535)
US 10689346 — method of use (U-4535)
US 10689346 — method of use (U-4535)
US 10689346 — method of use (U-4535)
US 10689346 — method of use (U-4535)
US 12590068 — drug substance
US 12590068 — drug substance
US 10329260 — drug substance
US 12552750 — drug substance
US 12590069 — drug substance
US 10329260 — drug substance
US 12545646 — drug substance
US 12590069 — drug substance
US 12545645 — drug substance
US 12545646 — drug substance
US 12545646 — drug substance
US 12545647 — drug substance
US 12116346 — drug substance
US 12116346 — drug substance
US 10329260 — drug substance
US 12545647 — drug substance
US 12545645 — drug substance
US 12552750 — drug substance
US 12590068 — drug substance
US 12545645 — drug substance
US 12545647 — drug substance
US 12545647 — drug substance
US 12552750 — drug substance
US 12552750 — drug substance
US 12590069 — drug substance
US 10329260 — drug substance
US 12116346 — drug substance
US 12545646 — drug substance
US 12545645 — drug substance
US 12590069 — drug substance
US 12116346 — drug substance
US 12590068 — drug substance
US 12590069*PED — drug product
US 12590069*PED — drug product
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US 12552750*PED — drug product
US 12545647*PED — drug product
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US 12545645*PED — drug product
US 12344585*PED — drug product
US 12344585*PED — drug product
US 12344585*PED — drug product
US 12344585*PED — drug product
US 11708333*PED — drug product
US 11708333*PED — drug product
US 11708333*PED — drug product
US 11708333*PED — drug product
US 10329260*PED — drug product
US 10329260*PED — drug product
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US 11618733*PED — drug product
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US 11117867*PED — drug product
US 11117867*PED — drug product
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US 11117867*PED — drug product
US 12116346*PED — drug product
US 12116346*PED — drug product
US 12116346*PED — drug product
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US 11230530*PED — drug product
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US 10125102*PED — drug product
US 10125102*PED — drug product
US 10125102*PED — drug product
US 10125102*PED — drug product
US 10662160*PED — drug product
US 10662160*PED — drug product
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US 10689346*PED — drug product
Exclusivity NP
Exclusivity NP
Exclusivity NP
Exclusivity NP
Exclusivity PED
Exclusivity PED
Exclusivity PED
Exclusivity PED
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 (128)
PatentTypeUse codeExpires
US 12344585 ↗ Method of use U-4535 Nov 1, 2039
US 12344585 ↗ Method of use U-4535 Nov 1, 2039
US 12344585 ↗ Method of use U-4535 Nov 1, 2039
US 12344585 ↗ Method of use U-4535 Nov 1, 2039
US 11708333 ↗ Method of use U-4535 Mar 9, 2035
US 11708333 ↗ Method of use U-4535 Mar 9, 2035
US 11708333 ↗ Method of use U-4535 Mar 9, 2035
US 11708333 ↗ Method of use U-4535 Mar 9, 2035
US 11618733 ↗ Method of use U-4535 Nov 1, 2039
US 11618733 ↗ Method of use U-4535 Nov 1, 2039
US 11618733 ↗ Method of use U-4535 Nov 1, 2039
US 11618733 ↗ Method of use U-4535 Nov 1, 2039
US 11117867 ↗ Method of use U-4535 Nov 1, 2039
US 11117867 ↗ Method of use U-4535 Nov 1, 2039
US 11117867 ↗ Method of use U-4535 Nov 1, 2039
US 11117867 ↗ Method of use U-4535 Nov 1, 2039
US 11230530 ↗ Method of use U-4535 Mar 9, 2035
US 11230530 ↗ Method of use U-4535 Mar 9, 2035
US 11230530 ↗ Method of use U-4535 Mar 9, 2035
US 11230530 ↗ Method of use U-4535 Mar 9, 2035
US 10125102 ↗ Drug substance U-4535 Apr 7, 2035
US 10125102 ↗ Drug substance U-4535 Apr 7, 2035
US 10125102 ↗ Drug substance U-4535 Apr 7, 2035
US 10125102 ↗ Drug substance U-4535 Apr 7, 2035
US 10662160 ↗ Drug substance U-4535 Nov 1, 2039
US 10662160 ↗ Drug substance U-4535 Nov 1, 2039
US 10662160 ↗ Drug substance U-4535 Nov 1, 2039
US 10662160 ↗ Drug substance U-4535 Nov 1, 2039
US 10689346 ↗ Method of use U-4535 Mar 9, 2035
US 10689346 ↗ Method of use U-4535 Mar 9, 2035
US 10689346 ↗ Method of use U-4535 Mar 9, 2035
US 10689346 ↗ Method of use U-4535 Mar 9, 2035
US 12590068 ↗ Drug substance — Nov 1, 2039
US 12590068 ↗ Drug substance — Nov 1, 2039
US 10329260 ↗ Drug substance — Mar 9, 2035
US 12552750 ↗ Drug substance — Nov 1, 2039
US 12590069 ↗ Drug substance — Nov 1, 2039
US 10329260 ↗ Drug substance — Mar 9, 2035
US 12545646 ↗ Drug substance — Nov 1, 2039
US 12590069 ↗ Drug substance — Nov 1, 2039
US 12545645 ↗ Drug substance — Nov 1, 2039
US 12545646 ↗ Drug substance — Nov 1, 2039
US 12545646 ↗ Drug substance — Nov 1, 2039
US 12545647 ↗ Drug substance — Nov 1, 2039
US 12116346 ↗ Drug substance — Mar 9, 2035
US 12116346 ↗ Drug substance — Mar 9, 2035
US 10329260 ↗ Drug substance — Mar 9, 2035
US 12545647 ↗ Drug substance — Nov 1, 2039
US 12545645 ↗ Drug substance — Nov 1, 2039
US 12552750 ↗ Drug substance — Nov 1, 2039
US 12590068 ↗ Drug substance — Nov 1, 2039
US 12545645 ↗ Drug substance — Nov 1, 2039
US 12545647 ↗ Drug substance — Nov 1, 2039
US 12545647 ↗ Drug substance — Nov 1, 2039
US 12552750 ↗ Drug substance — Nov 1, 2039
US 12552750 ↗ Drug substance — Nov 1, 2039
US 12590069 ↗ Drug substance — Nov 1, 2039
US 10329260 ↗ Drug substance — Mar 9, 2035
US 12116346 ↗ Drug substance — Mar 9, 2035
US 12545646 ↗ Drug substance — Nov 1, 2039
US 12545645 ↗ Drug substance — Nov 1, 2039
US 12590069 ↗ Drug substance — Nov 1, 2039
US 12116346 ↗ Drug substance — Mar 9, 2035
US 12590068 ↗ Drug substance — Nov 1, 2039
US 12590069*PED ↗ Drug product — May 1, 2040
US 12590069*PED ↗ Drug product — May 1, 2040
US 12590069*PED ↗ Drug product — May 1, 2040
US 12590069*PED ↗ Drug product — May 1, 2040
US 12590068*PED ↗ Drug product — May 1, 2040
US 12590068*PED ↗ Drug product — May 1, 2040
US 12590068*PED ↗ Drug product — May 1, 2040
US 12590068*PED ↗ Drug product — May 1, 2040
US 12552750*PED ↗ Drug product — May 1, 2040
US 12552750*PED ↗ Drug product — May 1, 2040
US 12552750*PED ↗ Drug product — May 1, 2040
US 12552750*PED ↗ Drug product — May 1, 2040
US 12545647*PED ↗ Drug product — May 1, 2040
US 12545647*PED ↗ Drug product — May 1, 2040
US 12545647*PED ↗ Drug product — May 1, 2040
US 12545647*PED ↗ Drug product — May 1, 2040
US 12545646*PED ↗ Drug product — May 1, 2040
US 12545646*PED ↗ Drug product — May 1, 2040
US 12545646*PED ↗ Drug product — May 1, 2040
US 12545646*PED ↗ Drug product — May 1, 2040
US 12545645*PED ↗ Drug product — May 1, 2040
US 12545645*PED ↗ Drug product — May 1, 2040
US 12545645*PED ↗ Drug product — May 1, 2040
US 12545645*PED ↗ Drug product — May 1, 2040
US 12344585*PED ↗ Drug product — May 1, 2040
US 12344585*PED ↗ Drug product — May 1, 2040
US 12344585*PED ↗ Drug product — May 1, 2040
US 12344585*PED ↗ Drug product — May 1, 2040
US 11708333*PED ↗ Drug product — Sep 9, 2035
US 11708333*PED ↗ Drug product — Sep 9, 2035
US 11708333*PED ↗ Drug product — Sep 9, 2035
US 11708333*PED ↗ Drug product — Sep 9, 2035
US 10329260*PED ↗ Drug product — Sep 9, 2035
US 10329260*PED ↗ Drug product — Sep 9, 2035
US 10329260*PED ↗ Drug product — Sep 9, 2035
US 10329260*PED ↗ Drug product — Sep 9, 2035
US 11618733*PED ↗ Drug product — May 1, 2040
US 11618733*PED ↗ Drug product — May 1, 2040
US 11618733*PED ↗ Drug product — May 1, 2040
US 11618733*PED ↗ Drug product — May 1, 2040
US 11117867*PED ↗ Drug product — May 1, 2040
US 11117867*PED ↗ Drug product — May 1, 2040
US 11117867*PED ↗ Drug product — May 1, 2040
US 11117867*PED ↗ Drug product — May 1, 2040
US 12116346*PED ↗ Drug product — Sep 9, 2035
US 12116346*PED ↗ Drug product — Sep 9, 2035
US 12116346*PED ↗ Drug product — Sep 9, 2035
US 12116346*PED ↗ Drug product — Sep 9, 2035
US 11230530*PED ↗ Drug product — Sep 9, 2035
US 11230530*PED ↗ Drug product — Sep 9, 2035
US 11230530*PED ↗ Drug product — Sep 9, 2035
US 11230530*PED ↗ Drug product — Sep 9, 2035
US 10125102*PED ↗ Drug product — Oct 7, 2035
US 10125102*PED ↗ Drug product — Oct 7, 2035
US 10125102*PED ↗ Drug product — Oct 7, 2035
US 10125102*PED ↗ Drug product — Oct 7, 2035
US 10662160*PED ↗ Drug product — May 1, 2040
US 10662160*PED ↗ Drug product — May 1, 2040
US 10662160*PED ↗ Drug product — May 1, 2040
US 10662160*PED ↗ Drug product — May 1, 2040
US 10689346*PED ↗ Drug product — Sep 9, 2035
US 10689346*PED ↗ Drug product — Sep 9, 2035
US 10689346*PED ↗ Drug product — Sep 9, 2035
US 10689346*PED ↗ Drug product — Sep 9, 2035
FDA exclusivity
CodeWhat it grantsExpires
NPNew ProductDec 11, 2028
NPNew ProductDec 11, 2028
NPNew ProductDec 11, 2028
NPNew ProductDec 11, 2028
PEDPediatric Exclusivity (+6 months)Jun 11, 2029
PEDPediatric Exclusivity (+6 months)Jun 11, 2029
PEDPediatric Exclusivity (+6 months)Jun 11, 2029
PEDPediatric Exclusivity (+6 months)Jun 11, 2029
Common questions
Is there a generic version of ORLADEYO 96 MG PELLET PACKET?
No FDA-approved generic equivalent is currently listed in the FDA Orange Book for ORLADEYO 96 MG PELLET PACKET. Based on the patents and exclusivity currently listed, the Orange Book estimate is that full-label generic entry may be delayed until May 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.

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

Medicare Part D (outpatient prescription) spending for Orladeyo — the program that covers self-administered drugs. 1 manufacturer.
⚠️ 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 Orladeyo. 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
$49.79M
Claims incl. refills
1K
Beneficiaries
349
Spend / beneficiary
$142,677.64
Spend / claim
$48,297.28
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.

📦 Packaging — all sizes for this product

Package NDCDescription Marketing startStatus
72769-0112-02 You're viewing this 4 DOSE PACK in 1 CARTON (72769-112-02) / 7 PACKET in 1 DOSE PACK / 16 PELLET in 1 PACKET 2025-12-12 Active

🧭 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 — Not published for this NDC Most self-administered / retail products have no J-code — that is normal.
Medicaid utilization (CMS SDUD) — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold.
“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 FDA registers it as 72769-112-02, which is what is printed on the packaging and shown on DailyMed. Insurance claims use a fixed 11-digit 5-4-2 format, so the short segment is padded with a leading zero: 72769-0112-02, written without dashes as 72769011202. The Identity section at the top of this page lists every form of this code.
What do the three segments of this NDC mean?
In 72769-0112-02, the first segment (72769) is the labeler code FDA assigned to BioCryst Pharmaceuticals, Inc.; the middle segment (0112) identifies this specific product — its ingredient, strength, and dosage form; and the last segment (02) identifies this exact package size and type. Together they name one specific package of one specific product.
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 BioCryst Pharmaceuticals, Inc.. Listing status can change — the directory data on this page refreshes weekly.
Who lists this product with the FDA?
BioCryst Pharmaceuticals, 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.
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.

📄 Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Jump with a chip, search within the label, or expand everything.
🎯 Indications and Usage ⏱️ Dosage and Administration 💊 Dosage Forms and Strengths ⛔ Contraindications ⚠️ Warnings and Cautions 🤒 Adverse Reactions 🔄 Drug Interactions 👥 Use in Specific Populations 🤰 Pregnancy 🧒 Pediatric Use 🧓 Geriatric Use 🧬 Clinical Pharmacology 🧬 Mechanism of Action 📦 How Supplied / Storage and Handling 📦 Storage and Handling 📋 Description 💬 Information for Patients
🎯 Indications and Usage 136 words ▾

1 INDICATIONS AND USAGE ORLADEYO ® is indicated for prophylaxis to prevent attacks of hereditary angioedema (HAE) in adults and pediatric patients 2 years of age and older. ORLADEYO is a plasma kallikrein inhibitor indicated for prophylaxis to prevent attacks of hereditary angioedema (HAE) in adults and pediatric patients 2 years and older. ( 1 ) Limitations of Use : ORLADEYO should not be used for treatment of acute HAE attacks.

( 1 ) Limitations of Use : The safety and effectiveness of ORLADEYO for the treatment of acute HAE attacks have not been established. ORLADEYO should not be used for treatment of acute HAE attacks. Additional doses or doses of ORLADEYO higher than the prescribed once-daily dose are not recommended due to the potential for QTc interval prolongation [see Warnings and Precautions (5.1) ] .

⏱️ Dosage and Administration ~3 min read ▾

2 DOSAGE AND ADMINISTRATION Recommended dosage in adult and pediatric patients aged 12 years and older: 150 mg capsule orally once daily with food. ( 2.1 ) Recommended dosage in pediatric patients aged 2 to less than 12 years is based on body weight as follows ( 2.2 , 2.5 ): Weight Recommended Dosage (oral pellets) Administration Instructions 12 kg to less than 24 kg 72 mg once daily Pour directly in mouth and swallow immediately with non-acidic liquid, or, Sprinkle over 1 tablespoon (15 mL) of non-acidic soft food and consume immediately.

A meal should be consumed just before or after administration. 24 kg to less than 32 kg 96 mg once daily 32 kg to less than 40 kg 108 mg once daily 40 kg or greater 132 mg once daily See full prescribing information for recommended dosage in patients with hepatic impairment and dosage modification in patients with persistent gastrointestinal adverse reactions. ( 2.3 , 2.4 )

2.1Recommended Dosage in Adults and Pediatric Patients 12 Years of Age and Older The recommended dosage of ORLADEYO capsules for adults and pediatric patients 12 years of age and older is 150 mg taken orally once daily with food.

2.2Recommended Dosage in Pediatric Patients 2 Years to Less than 12 Years of Age The recommended dosage of ORLADEYO oral pellets for pediatric patients 2 years to less than 12 years of age is based on the patient's body weight as provided in Table 1. Take ORLADEYO orally with food (a meal should be consumed just before or after dosing) [see Dosage and Administration (2.5) ] . Table 1: Recommended Dosage of ORLADEYO Oral Pellets by Body Weight in Pediatric Patients 2 Years to Less than 12 Years of Age Body Weight (kg) Recommended Dosage of ORLADEYO Oral Pellets 12 kg to less than 24 kg 72 mg (one packet) once daily 24 kg to less than 32 kg 96 mg (one packet) once daily 32 kg to less than 40 kg 108 mg (one packet) once daily 40 kg or greater 132 mg (one packet) once daily

2.3Recommended Dosage in Patients with Hepatic Impairment Mild Hepatic Impairment (Child-Pugh Class A) Adult and Pediatric Patients 2 Years of Age and Older No dosage modification of ORLADEYO is recommended [see Use in Specific Populations (8.7) and Clinical Pharmacology (12.3) ] . Moderate or Severe Hepatic Impairment (Child-Pugh Class B or C) Adult and Pediatric Patients 12 Years of Age and Older Recommended dosage of ORLADEYO capsules is 110 mg taken orally once daily with food [see Use in Specific Populations (8.7) and Clinical Pharmacology (12.3) ] .

Pediatric Patients 2 Years to Less than 12 Years of Age Avoid use of ORLADEYO [see Use in Specific Populations (8.7) ] .

2.4Dosage Modification in Patients with Persistent GI Adverse Reactions Gastrointestinal (GI) reactions may occur in patients receiving ORLADEYO [see Adverse Reactions (6.1) ] . For adults and pediatric patients 12 years of age and older, if GI adverse reactions persist, consider a lower ORLADEYO capsules dosage of 110 mg once daily with food. For pediatric patients 2 to less than 12 years of age with persistent GI adverse reactions, consider the risks and benefits of continuing treatment with ORLADEYO.

2.5Administration Instructions for Oral Pellets Do not chew or crush ORLADEYO oral pellets because this will affect the film coating (taste masking) and result in bitter taste. Administer one packet of oral pellets as follows: Pour the entire contents of one packet directly into the mouth and swallow immediately with non-acidic liquid (e.g., water or milk). OR Sprinkle the entire contents of one packet over approximately one tablespoon (15 mL) of soft, non-acidic food and consume immediately.

Food should be at or below room temperature. Examples of soft, non-acidic foods include pudding, mashed potatoes, creamed corn, pureed peas, pureed bananas, and pureed carrots. Acidic foods such as yogurt and applesauce should not be used because they can dissolve the film coating (taste masking) and result in a bitter taste .

The film coating (taste masking) remains i…

💊 Dosage Forms and Strengths 94 words ▾

3 DOSAGE FORMS AND STRENGTHS Capsules: 150 mg, 110 mg ( 3 ) Oral Pellets: 72 mg, 96 mg, 108 mg, or 132 mg in unit-dose packets ( 3 ) Capsules: 150 mg: a white opaque body with a black imprint "150" and a light blue opaque cap with a black imprint "BCX". 110 mg: light blue opaque body and cap with a white imprint "110" on body and a white imprint "BCX" on cap. Oral Pellets: 72 mg, 96 mg, 108 mg, or 132 mg, white to off-white film-coated pellets in unit-dose packets.

⛔ Contraindications 7 words ▾

4 CONTRAINDICATIONS None. None. ( 4 )

⚠️ Warnings and Cautions 103 words ▾

5 WARNINGS AND PRECAUTIONS An increase in QTc interval prolongation can occur at dosages higher than the recommended dosage. Additional doses or doses of ORLADEYO higher than the recommended dosage are not recommended. ( 5.1 )

5.1Risk of QTc Interval Prolongation with Higher-Than-Recommended Dosages ORLADEYO should not be used for treatment of acute attacks of HAE. Additional doses or doses of ORLADEYO higher than the recommended dosage are not recommended. An increase in QTc interval was observed in adults at dosages higher than 150 mg once daily and was concentration dependent [see Dosage and Administration (2) and Clinical Pharmacology (12.2) ] .

🤒 Adverse Reactions ~3 min read ▾

6 ADVERSE REACTIONS The following clinically significant adverse reaction is described elsewhere in the labeling: QTc Interval Prolongation [see Warnings and Precautions (5.1) ] . Most common adverse reactions (≥10%) are abdominal pain, vomiting, diarrhea, back pain, and gastroesophageal reflux disease. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact BioCryst Pharmaceuticals, Inc. at 1-833-633-2279 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. Adverse Reactions in Adult and Pediatric Patients 12 Years of Age and Older The safety of ORLADEYO is primarily based on 24-week (Part 1) data from a 3-part, double-blind, parallel-group, placebo-controlled trial (Trial 1) in 120 patients with Type I or II HAE who were randomized and dosed with either ORLADEYO 110 mg, 150 mg, or placebo, once daily with food.

After Week 24, patients who continued in the study received active treatment through 48 weeks. In Trial 1, a total of 81 patients aged 12 years and older with HAE received at least one dose of ORLADEYO in Part 1. Overall, 66% of patients were female and 93% of patients were White with a mean age of 41.6 years.

The proportion of patients who discontinued study drug prematurely due to adverse reactions was 7% and 3% for patients treated with ORLADEYO 110 mg and 150 mg, respectively, and 3% for placebo-treated patients. No deaths occurred in the trial. The safety profile of ORLADEYO was generally similar across all subgroups of patients, including analysis by age, sex, and geographic region.

Table 2 shows adverse reactions occurring in ≥10% of adult and pediatric patients aged 12 years and older in any ORLADEYO treatment group that also occurred at a higher rate than in the placebo treatment group in Trial 1. Table 2: Adverse Reactions Observed in ≥10% of Adult and Pediatric Patients Aged 12 Years and Older with HAE in Any ORLADEYO Treatment Group (Trial 1) Adverse Reaction Placebo (N=39) ORLADEYO 110 mg (N=41) 150 mg (N=40) Total (N=81) n (%) n (%) n (%) n (%) Abdominal Pain includes Abdominal pain, Abdominal discomfort, Abdominal pain upper, and Abdominal tenderness 4 (10) 4 (10) 9 (23) 13 (16) Vomiting 1 (3) 4 (10) 6 (15) 10 (12) Diarrhea includes Diarrhea and Frequent bowel movements 0 4 (10) 6 (15) 10 (12) Back Pain 1 (3) 1 (2) 4 (10) 5 (6) Gastroesophageal Reflux Disease 0 4 (10) 2 (5) 6 (7) Gastrointestinal adverse reactions, including abdominal pain, vomiting, and diarrhea occurred more frequently in patients receiving ORLADEYO 150 mg versus ORLADEYO 110 mg or placebo.

These adverse reactions generally occurred early after initiation of treatment with ORLADEYO, became less frequent with time, and typically self-resolved. No patients in the ORLADEYO 150 mg dose group and 1 patient in the ORLADEYO 110 mg dose group discontinued treatment due to a gastrointestinal adverse reaction. Less Common Adverse Reactions Other adverse reactions that occurred in Part 1 of Trial 1 with an incidence between 5% to <10% and at a higher incidence in ORLADEYO-treated patients compared to placebo-treated patients included headache (9% versus 5%), fatigue (6% versus 3%), and flatulence (6% versus 3%).

A maculopapular drug rash was reported in less than 1% of patients treated with ORLADEYO. The rash resolved, including in patients who continued dosing. Safety data are also available from 227 patients enrolled in an ongoing, open-label, long-term safety study (Trial 2) who received ORLADEYO 110 mg (N=100) or 150 mg (N=127) once daily with food and are consistent with the 24-week controlled safety data from Trial 1 (Part 1).

Laboratory Abnormalities Transaminase Elevations In Part 1 of Trial 1, one patient treated with ORLADEYO 150 mg discontinued trea…

🔄 Drug Interactions ~2 min read ▾

7 DRUG INTERACTIONS P-gp inducers: Avoid use with ORLADEYO. ( 7.1 ) CYP2D6, CYP3A4 or P-gp Substrates: When used concomitantly with ORLADEYO, closely monitor or modify the dosage of the substrates where minimal increases in concentration may lead to serious adverse reactions. ( 7.2 , 12.3 )

7.1Effect of Other Drugs on ORLADEYO P-gp Inducers Berotralstat is a substrate of P-gp and BCRP. P-gp inducers may decrease berotralstat plasma concentration, leading to reduced efficacy of ORLADEYO. Avoid concomitant use of P-gp inducers with ORLADEYO.

7.2Effect of ORLADEYO on Other Drugs CYP2D6 and CYP3A4 Substrates ORLADEYO at a dose of 150 mg is a moderate inhibitor of CYP2D6 and CYP3A4. Concomitant use of ORLADEYO with CYP2D6 or CYP3A4 substrates can increase exposure of the CYP2D6 or CYP3A4 substrates and may increase the risk of adverse reactions associated with the substrates. If ORLADEYO is concomitantly used with CYP2D6 or CYP3A4 substrates where minimal increases in the concentration of the substrates may lead to serious adverse reactions, closely monitor or modify the dosage of the CYP2D6 or CYP3A4 substrate [see Clinical Pharmacology (12.3) ] .

Refer to the Prescribing Information of the CYP2D6 or CYP3A4 substrate. Desogestrel Concomitant use of ORLADEYO with desogestrel increases exposure to etonogestrel, the active metabolite of desogestrel, and may increase the risk of desogestrel-associated adverse reactions. Consider the benefits and risks when using ORLADEYO concomitantly with desogestrel [see Clinical Pharmacology (12.3) ] .

P-gp Substrates ORLADEYO at 2-times the maximum recommended dose of 150 mg is a P-gp inhibitor and can increase exposure of P-gp substrates, leading to increased risk of adverse reactions associated with the substrates. Higher-than-recommended dosages of ORLADEYO are not recommended [see Warnings and Precautions (5.1) ] . If ORLADEYO is concomitantly used with P-gp substrates where minimal increases in the concentration of the substrates may lead to serious adverse reactions, closely monitor or modify the dosage of the P-gp substrate [see Clinical Pharmacology (12.3) ] .

Refer to the Prescribing Information of the P-gp substrate.

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS Avoid use of ORLADEYO in pediatric patients 2 years to less than 12 years of age with severe renal impairment. ( 8.6 ) ORLADEYO is not recommended in patients with end-stage renal disease. ( 8.6 )

8.1Pregnancy Risk Summary There are insufficient data in pregnant women available to inform drug-related risks with ORLADEYO use in pregnancy. Based on animal reproduction studies, no evidence of structural alterations was observed when berotralstat was administered orally to pregnant rats and rabbits during organogenesis at doses up to approximately 10- and 2-times, respectively, the maximum recommended human daily dose (MRHDD) in adults on an AUC basis (see Data ) . The 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% to 4% and 15% to 20%, respectively. Data Animal Data In animal reproduction studies, oral administration of berotralstat to pregnant rats and rabbits during the period of organogenesis did not cause fetal structural alterations. The berotralstat dose in rats and rabbits was up to approximately 10- and 2-times, respectively, the MRHDD in adults (on an AUC basis at maternal doses of 75 and 100 mg/kg/day, respectively).

In a pre- and postnatal development study in rats, oral administration of berotralstat to pregnant rats during the period of organogenesis and until delivery at doses up to 45 mg/kg/day (approximately 2-times of the MRHDD on a mg/m 2 basis) did not cause fetal structural alterations either. Berotralstat concentrations in the fetal blood were approximately 5% to 11% of the maternal blood.

8.2Lactation Risk Summary There are no data on the presence of berotralstat in human milk, its effects on the breastfed infant, or its effects on milk production. However, when a drug is present in animal milk, it is likely that the drug will be present in human milk. Low levels of berotralstat were detected in the plasma of rat pups when dams were dosed with the drug orally during the lactation period.

The berotralstat concentration in the pup plasma was approximately 2% of the maternal plasma (see Data ) . The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for ORLADEYO and any potential adverse effects on the breastfed infant from ORLADEYO or from the underlying maternal condition. Data Animal Data In the pre- and post-natal development study in rats, berotralstat was administered to dams during the pregnancy and lactation periods at doses up to 45 mg/kg/day (approximately 2-times of the MRHDD on a mg/m 2 basis).

Berotralstat was detected in the plasma of pups during the lactation period. The berotralstat concentration in the pup plasma was approximately 2% of the maternal plasma. Both dams and pups at 45 mg/kg/day showed statistically significant decreases in body weight gain (p<0.05).

No treatment-related effects were observed at 25 mg/kg/day (approximately equal to the MRHDD on a mg/m 2 basis).

8.4Pediatric Use The safety and effectiveness of ORLADEYO for prophylaxis to prevent attacks of hereditary angioedema have been established in pediatric patients aged 2 and older. The use of ORLADEYO in pediatric patients aged 12 to <18 years with HAE is supported by evidence from an adequate and well-controlled trial (Trial 1) that included adults and a total of 6 pediatric patients aged 12 to <18 years. The safety profile and attack rate in the study were similar to those observed in adults [see Adverse Reactions (6.1) , Clinical Pharmacology (12.3) , and Clinical Studies (14) ] .

An additional 10 pediatric patients aged 12 to <18 years were enrolled in the open-label study (Trial 2). The use of ORLADEYO in pediatric patients aged 2 to <12 years with HAE is supported by efficacy data from an adequate and well-controlled study in adults and ped…

🤰 Pregnancy ~1 min read ▾

8.1Pregnancy Risk Summary There are insufficient data in pregnant women available to inform drug-related risks with ORLADEYO use in pregnancy. Based on animal reproduction studies, no evidence of structural alterations was observed when berotralstat was administered orally to pregnant rats and rabbits during organogenesis at doses up to approximately 10- and 2-times, respectively, the maximum recommended human daily dose (MRHDD) in adults on an AUC basis (see Data ) . The 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% to 4% and 15% to 20%, respectively. Data Animal Data In animal reproduction studies, oral administration of berotralstat to pregnant rats and rabbits during the period of organogenesis did not cause fetal structural alterations. The berotralstat dose in rats and rabbits was up to approximately 10- and 2-times, respectively, the MRHDD in adults (on an AUC basis at maternal doses of 75 and 100 mg/kg/day, respectively).

In a pre- and postnatal development study in rats, oral administration of berotralstat to pregnant rats during the period of organogenesis and until delivery at doses up to 45 mg/kg/day (approximately 2-times of the MRHDD on a mg/m 2 basis) did not cause fetal structural alterations either. Berotralstat concentrations in the fetal blood were approximately 5% to 11% of the maternal blood.

🧒 Pediatric Use ~1 min read ▾

8.4Pediatric Use The safety and effectiveness of ORLADEYO for prophylaxis to prevent attacks of hereditary angioedema have been established in pediatric patients aged 2 and older. The use of ORLADEYO in pediatric patients aged 12 to <18 years with HAE is supported by evidence from an adequate and well-controlled trial (Trial 1) that included adults and a total of 6 pediatric patients aged 12 to <18 years. The safety profile and attack rate in the study were similar to those observed in adults [see Adverse Reactions (6.1) , Clinical Pharmacology (12.3) , and Clinical Studies (14) ] .

An additional 10 pediatric patients aged 12 to <18 years were enrolled in the open-label study (Trial 2). The use of ORLADEYO in pediatric patients aged 2 to <12 years with HAE is supported by efficacy data from an adequate and well-controlled study in adults and pediatric patients aged 12 years and older (Trial 1), and pharmacokinetic and safety data from 29 pediatric patients aged 2 to less than 12 years enrolled in a multicenter, single-arm, open-label study with additional support from population pharmacokinetic analyses.

Pediatric patients aged 2 to less than 12 years received a dosage of ORLADEYO based on the patient's body weight, which showed no clinically significant difference in drug exposures from those observed in adults treated with ORLADEYO 150 mg [see Clinical Pharmacology (12.3) ] . Pediatric patients aged 2 to less than 12 years were treated for at least 12 weeks, with 17 patients completing 48 weeks of treatment. No new safety signals were observed in pediatric patients aged 2 to less than 12 years [see Adverse Reactions (6.1) ] .

The safety and effectiveness of ORLADEYO have not been established in pediatric patients younger than 2 years of age.

🧓 Geriatric Use 81 words ▾

8.5Geriatric Use Of the total number of patients in clinical studies of ORLADEYO, 9 patients were 65 years of age and over in Trial 1, and 5 patients were 65 years of age and over in Trial 2 (open-label safety study). No overall differences in safety or effectiveness of ORLADEYO have been observed between patients 65 years of age and older and younger adult patients [see Adverse Reactions (6.1) , Clinical Pharmacology (12.3) , and Clinical Studies (14) ] .

🧬 Clinical Pharmacology ~3 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action Berotralstat is a plasma kallikrein inhibitor that binds to plasma kallikrein and inhibits its proteolytic activity. Plasma kallikrein is a protease that cleaves high-molecular-weight kininogen (HMWK) to generate cleaved HMWK (cHMWK) and bradykinin, a potent vasodilator that increases vascular permeability resulting in swelling and pain associated with HAE. In patients with HAE due to C1-inhibitor (C1-INH) deficiency or dysfunction, normal regulation of plasma kallikrein activity is not present, which leads to uncontrolled increases in plasma kallikrein activity and results in angioedema attacks.

Berotralstat decreases plasma kallikrein activity to control excess bradykinin generation in patients with HAE.

12.2Pharmacodynamics Concentration-dependent inhibition of plasma kallikrein, measured as a reduction from baseline of specific enzyme activity, was demonstrated after oral administration of ORLADEYO once daily in patients with HAE. Cardiac Electrophysiology At the maximum recommended dosage of 150 mg once daily in adults, clinically significant QTc interval prolongation was not observed. At 3-times the maximum recommended dosage, the mean (upper 90% confidence interval) increase in QTcF was 15.9 msec (23.5 msec).

The observed increase in QTcF was concentration dependent.

12.3Pharmacokinetics Following oral administration of berotralstat 150 mg once daily in adults, the geometric mean steady-state C max is 158 ng/mL (range: 110 to 234 ng/mL) and steady-state area under the curve over the dosing interval (AUC tau ) is 2770 ng*hr/mL (range: 1880 to 3790 ng*hr/mL). Following oral administration of berotralstat 110 mg once daily, the geometric mean steady-state C max is 97.8 ng/mL (range: 63 to 235 ng/mL) and steady-state AUC tau is 1600 ng*hr/mL (range: 950 to 4170 ng*hr/mL). Berotralstat exposure (C max and AUC) increases in a greater than dose-proportional manner and steady state is reached in approximately 6 to 12 days.

Berotralstat accumulation at steady state is approximately 5-fold at the recommended dosage. No clinically significant difference in the pharmacokinetics of berotralstat was observed between healthy adult subjects and patients with HAE. Absorption The median time to maximum plasma concentration (T max ) of berotralstat when administered with food is 5 hours (range: 1 to 8 hours).

No clinically significant difference in ORLADEYO exposure was observed following oral administration of either the pellets or capsules at the recommended adult dosage for 7 days. Effect of Food No clinically significant differences in the C max and AUC of berotralstat were observed following administration with a high-fat meal, however the median T max was delayed by 3 hours, from 2 hours (fasted) to 5 hours (fed). Distribution Plasma protein binding is approximately 99%.

After a single dose of radiolabeled berotralstat at 2-times the maximum recommended dosage of 150 mg, the blood to plasma ratio was approximately 0.92. Elimination The median elimination half-life of berotralstat is approximately 93 hours (range: 39 to 152 hours). Metabolism Berotralstat is metabolized by CYP2D6 and by CYP3A4 with low turnover in vitro .

After a single oral dose of radiolabeled berotralstat at 2-times the maximum recommended dosage of 150 mg, berotralstat represented 34% of the total plasma radioactivity, with 8 metabolites, each accounting for between 1.8 and 7.8% of the total radioactivity. Excretion After a single oral dose of radiolabeled berotralstat at 2-times the maximum recommended dosage of 150 mg, approximately 9% was excreted in urine (3.4% unchanged; range: 1.8 to 4.7%) and 79% was excreted in feces. Specific Populations In adults and pediatric patients 12 to <18 years of age, no clinically significant differences in the pharmacokinetics of ORLADEYO were observed based on age (12 to 74 years), sex, race, and body weight.

Pediatric Patients Based on population pharmacokinetic analyses th…

🧬 Mechanism of Action 100 words ▾

12.1Mechanism of Action Berotralstat is a plasma kallikrein inhibitor that binds to plasma kallikrein and inhibits its proteolytic activity. Plasma kallikrein is a protease that cleaves high-molecular-weight kininogen (HMWK) to generate cleaved HMWK (cHMWK) and bradykinin, a potent vasodilator that increases vascular permeability resulting in swelling and pain associated with HAE. In patients with HAE due to C1-inhibitor (C1-INH) deficiency or dysfunction, normal regulation of plasma kallikrein activity is not present, which leads to uncontrolled increases in plasma kallikrein activity and results in angioedema attacks.

Berotralstat decreases plasma kallikrein activity to control excess bradykinin generation in patients with HAE.

📦 How Supplied / Storage and Handling 195 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING ORLADEYO (berotralstat) capsules and oral pellets are supplied as follows in Table 4: Table 4. Dosage Form, Strength, and Package Configuration for ORLADEYO Dosage Form Strength Description Package Configuration NDC Capsule 110 mg light blue opaque body and cap with a white imprint "110" on body and a white imprint "BCX" on cap A 28-day supply of ORLADEYO is provided in a carton containing 4 child-resistant shellpacks, each containing a 7-capsule blister card. Each carton contains a tamper-evident seal.

Do not use if tamper-evident seal is broken or missing. 72769-102-01 150 mg white opaque body with a black imprint "150" and a light blue opaque cap with a black imprint "BCX" 72769-101-01 Pellets 72 mg white to off-white, film-coated pellets A 28-day supply of ORLADEYO oral pellets is provided in a carton containing 4 wallets, each containing 7 child-resistant unit-dose packets. Each carton contains a tamper-evident seal.

Do not use if tamper-evident seal is broken or missing. 72769-111-02 96 mg 72769-112-02 108 mg 72769-113-02 132 mg 72769-114-02 Store at 20°C to 25°C (68°F to 77°F). Excursions permitted between 15°C and 30°C (59°F to 86°F) [see USP Controlled Room Temperature] .

📦 Storage and Handling 23 words ▾

Store at 20°C to 25°C (68°F to 77°F). Excursions permitted between 15°C and 30°C (59°F to 86°F) [see USP Controlled Room Temperature] .

📋 Description ~1 min read ▾

11 DESCRIPTION ORLADEYO (berotralstat) is a plasma kallikrein inhibitor. Berotralstat is presented as the dihydrochloride salt with the chemical name 1-[3-(aminomethyl)phenyl]- N -(5-{( R )-(3-cyanophenyl)[(cyclopropylmethyl)amino]methyl}-2-fluorophenyl)-3-(trifluoromethyl)-1 H -pyrazole-5-carboxamide dihydrochloride. The chemical structure is: Berotralstat dihydrochloride is a white to off-white powder that is soluble in water at pH ≤4.

The molecular formula is C 30 H 26 F 4 N 6 O ∙ 2HCl and the molecular weight is 635.49 (dihydrochloride). ORLADEYO (berotralstat) capsules contain 150 mg of berotralstat (equivalent to 169.4 mg berotralstat dihydrochloride) or 110 mg of berotralstat (equivalent to 124.3 mg berotralstat dihydrochloride) in hard gelatin capsules for oral administration. Each capsule contains the active ingredient berotralstat dihydrochloride and the inactive ingredients colloidal silicon dioxide, crospovidone, magnesium stearate, and pregelatinized starch.

ORLADEYO (berotralstat) oral pellets are white to off-white film-coated pellets for oral administration and enclosed in a unit-dose packet containing berotralstat 72 mg (equivalent to 81.3 mg berotralstat dihydrochloride), 96 mg (equivalent to 108.4 mg berotralstat dihydrochloride), 108 mg (equivalent to 122.0 mg berotralstat dihydrochloride), or 132 mg (equivalent to 149.1 mg of berotralstat dihydrochloride). Each unit-dose packet contains the active ingredient berotralstat dihydrochloride and the inactive ingredients colloidal silicon dioxide, crospovidone, magnesium stearate, and pregelatinized starch.

The oral pellets film coating contains butylated methacrylate copolymer, silicon dioxide, sodium lauryl sulphate, stearic acid, talc, and titanium dioxide. Chemical Structure

💬 Information for Patients ~1 min read ▾

17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information). Inform patients of the risks and benefits of ORLADEYO before prescribing or administering to the patient. Not for Acute Treatment of HAE Attacks Advise patients to take their usual rescue medication to treat an acute attack of HAE.

Inform patients that the safety and effectiveness of ORLADEYO has not been established as a treatment for acute HAE attacks [see Indications and Usage (1) ] . QTc Prolongation with Higher Than Recommended Dosages Advise patients that they should not take daily doses higher than their prescribed once-daily dose or additional doses of ORLADEYO to treat an acute attack of HAE due to risk of QTc interval prolongation [see Indications and Usage (1) and Warnings and Precautions (5.1) ] . Administration Instructions for Oral Pellets Instruct patients that ORLADEYO oral pellets should not be chewed or crushed because this will affect the film coating, which masks the bitter taste.

Advise patients to take ORLADEYO oral pellets by pouring one packet directly into the mouth and swallowing with a non-acidic liquid (e.g., water or milk), or to sprinkle one packet over one tablespoon of soft, non-acidic food and consume immediately [see Dosage and Administration (2.5) ] . Drug Interactions Advise patients that ORLADEYO may interact with other drugs [see Drug Interactions (7) and Clinical Pharmacology (12.3) ] . Advise patients to report to their healthcare provider the use of any other prescription or nonprescription medication or herbal products.

Source: FDA Structured Product Labeling, mirrored from DailyMed / openFDA. Prefer the government’s original formatting? View this label on DailyMed ↗
← 72769-0111-02 · BioCryst 72769-0113-02 · BioCryst →
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.