FDA-filed SPL labeling · retrieved through openFDA

Fostemsavir

Fostemsavir is an HIV-1 attachment inhibitor used, in combination with other antiretroviral medicines, to treat HIV-1 infection in heavily treatment-experienced adults whose virus has become resistant to multiple other therapies.

Brand name Rukobia
Rx Form 1 Route Oral
Dr. Brian Staiger, PharmD, BCPS
Reviewed by Last reviewed Jul 10, 2026
🧬 Where this information comes from Click to expand

The clinical label records used on this page are FDA-filed Structured Product Labeling (SPL) retrieved through openFDA. We identified 1 clinical label set within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. Forms, routes, brands, labelers, strengths, and NDC product-record counts are built separately from matching FDA National Drug Code Directory records. The linked DailyMed document is a representative official source for verification, not the page’s only clinical source. View the linked label on DailyMed →

At a glance
Linked label effectiveFeb 13, 2024
AvailabilityRx
Earliest approval/marketing year ⓘ2020
FDA-listed product records ⓘ4
Boxed warningNone found in compared labels
How we combine label and product data →
✓No current FDA shortage listed · checked Sep 24, 2026
⭐ Fostemsavir at a glance The quick version — the full detail is in the Patient Information Guide below.
💊
HelloPharmacist Editorial Team Bottom Line
Fostemsavir (Rukobia) is a last-resort HIV-1 treatment reserved for adults who have run out of options with other antiretroviral regimens due to drug resistance or tolerability issues. It works by a unique mechanism — blocking HIV from attaching to immune cells — making it valuable when most other HIV drugs have stopped working. It must always be combined with other antiretrovirals, and several common drugs are off-limits with it due to serious interactions.

📖 Fostemsavir: Patient Information Guide

A plain-language walkthrough of Fostemsavir — what it treats, how it works, how it’s taken, side effects, warnings and interactions. Tap any section to expand it.

🎯What it's used for▾

Fostemsavir is used to treat HIV-1 infection in adults who have exhausted many prior treatment options. Here is what the FDA-approved evidence supports:

  • Rukobia (fostemsavir extended-release tablet), taken by mouth in combination with other antiretroviral medicines, is approved for HIV-1 infection in heavily treatment-experienced adults with multidrug-resistant HIV-1 whose current regimen is failing — due to resistance, intolerance, or safety issues.
⚙️How it works▾

Fostemsavir is a prodrug, meaning it is inactive until the body converts it into its active form, temsavir. Temsavir is an HIV-1 attachment inhibitor — it binds to a protein on HIV's outer coat called gp120, which the virus normally uses to grab onto and enter CD4+ T cells (key immune cells). By blocking that attachment step, temsavir prevents the virus from getting inside the cell and making copies of itself.

This mechanism is distinct from most other HIV drugs, which act at later stages of the viral life cycle. That's why it can be effective even when the virus has developed resistance to multiple other antiretroviral classes. However, certain HIV subtypes — particularly subtype AE, common in Southeast Asia — show naturally reduced sensitivity to temsavir.

💊How it's taken▾

Rukobia extended-release tablets are taken by mouth twice daily, with or without food. The tablets must be swallowed whole — do not chew, crush, or split them, as this can affect how the medicine is released. Always take Rukobia alongside other antiretroviral medicines as prescribed.

  • Can be taken with or without food at a standard meal; a high-fat meal significantly increases drug exposure, so consistency in how you take it may be helpful
  • Swallow tablets whole — do not crush, chew, or split
  • No dose adjustment is needed for kidney problems or liver impairment
🤒Side effects — in detail▾

Most side effects reported with Rukobia are mild to moderate. Common ones include:

  • Nausea
  • Diarrhea
  • Headache
  • Stomach pain or discomfort
  • Upset stomach (dyspepsia)
  • Fatigue or weakness
  • Rash
  • Sleep disturbances
  • Drowsiness (somnolence)
  • Vomiting

Serious reactions to watch for include signs of immune reconstitution syndrome (new or worsening infections or inflammation after starting therapy), liver enzyme elevations (especially with hepatitis B or C co-infection), and heart rhythm changes. Contact your doctor right away if you notice jaundice, severe fatigue, irregular heartbeat, or sudden flares of illness.

⚠️Warnings & precautions▾
  • Immune reconstitution syndrome: As your immune system recovers with HIV treatment, it can overreact to previously hidden infections (like tuberculosis, CMV, or PCP), causing inflammation. Autoimmune conditions (e.g., Graves' disease, Guillain-Barré syndrome) can also emerge, sometimes months after starting therapy.
  • Heart rhythm (QTc prolongation): Very high doses of Rukobia significantly prolong the QT interval — a measure of heart electrical activity — raising the risk of a dangerous arrhythmia called Torsade de Pointes. Use with caution if you have a history of QT prolongation, heart disease, or if you take other QT-prolonging drugs. Elderly patients are more vulnerable.
  • Liver enzyme elevations with hepatitis co-infection: If you also have hepatitis B or C, your liver enzymes should be monitored regularly. Some cases reflected hepatitis B reactivation, especially when anti-hepatitis therapy was stopped.
  • Drug interactions causing loss of HIV control: Several common medicines can dramatically lower Rukobia's effectiveness. Using Rukobia with strong CYP3A inducers can cause the HIV treatment to fail entirely.
🔀What it interacts with▾

Fostemsavir interacts with a number of commonly used medicines. Key interactions to know about:

  • Strong CYP3A inducers (rifampin, carbamazepine, phenytoin, enzalutamide, mitotane, St. John's wort) — contraindicated; these drugs lower temsavir levels enough to cause HIV treatment failure
  • Hepatitis C antivirals grazoprevir and voxilaprevir — Rukobia raises their levels, increasing risk of liver enzyme elevations; switch to an alternative HCV regimen if possible
  • Ethinyl estradiol-containing oral contraceptives — Rukobia raises estrogen levels; limit daily ethinyl estradiol to no more than 30 mcg and be extra cautious if you have risk factors for blood clots
  • Statins (rosuvastatin, atorvastatin, fluvastatin, pitavastatin, simvastatin) — Rukobia increases statin exposure; use the lowest effective statin dose and monitor for muscle pain or weakness
  • QT-prolonging drugs — combining with Rukobia may add to the risk of dangerous heart rhythm problems; use with caution

This is not a complete list of interactions. Always talk with your doctor or pharmacist before starting, stopping, or changing any medication.

📋Before taking it▾
  • Do not take Rukobia if you have had a serious allergic reaction to fostemsavir or any component of the tablet
  • Do not take Rukobia with strong CYP3A inducers (rifampin, carbamazepine, phenytoin, enzalutamide, mitotane, St. John's wort) — this combination is contraindicated
  • Tell your doctor if you have hepatitis B or C — liver monitoring is recommended throughout treatment
  • Tell your doctor about any heart conditions or history of QT interval prolongation before starting
  • Tell your doctor about all medicines, vitamins, and herbal supplements you take
  • Pregnancy: Human safety data are limited; animal studies showed fetal harm at very high doses. A pregnancy registry exists — call 1-800-258-4263 if you become pregnant while taking Rukobia
  • Breastfeeding: Not recommended — HIV can be passed through breast milk, and drug exposure to the infant is also a concern
  • Children: Safety and effectiveness in pediatric patients have not been established
  • Older adults: Use with extra caution — elderly patients are more susceptible to QT interval effects and may have reduced kidney, liver, or heart function
  • No dose adjustment is needed for kidney impairment, hemodialysis, or mild to severe liver impairment
🚑If you take too much▾

There is no specific antidote for a Rukobia overdose. If too much is taken, the heart rhythm (QT interval) should be monitored along with vital signs and overall clinical status. Because fostemsavir binds strongly to proteins in the blood, dialysis is unlikely to remove a meaningful amount of the drug.

📡Pharmacodynamics — effects in the body▾

At the recommended dose, Rukobia does not meaningfully prolong the QT interval — a measure of heart electrical activity. However, at four times the recommended daily dose, a clinically significant QT prolongation was observed, and the degree of prolongation tracked with temsavir blood levels. This means the heart rhythm risk is dose-dependent, which is why staying at the prescribed dose matters.

🔬Pharmacokinetics — how your body processes it▾

Fostemsavir is a prodrug that converts rapidly to its active form, temsavir, after being swallowed — fostemsavir itself is generally undetectable in the bloodstream. Temsavir reaches peak blood levels in about 2 hours and has a half-life of around 11 hours, supporting twice-daily dosing. It is primarily broken down by the liver (through esterases and the CYP3A4 enzyme pathway) and is about 88% bound to proteins in the blood. A high-fat meal substantially increases drug exposure compared to fasting, so consistency in how the medicine is taken may be relevant.

📦How to store it▾

Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F) .

📄 Written from Fostemsavir’s FDA-approved label information, summarized in plain language with AI, and reviewed by our pharmacy team before publication. Every point is grounded in that labeling — nothing is invented. How we use AI →

146

Supplements & herbs that interact with Fostemsavir

146 supplements and herbal products have documented interactions with Fostemsavir in the licensed clinical database we use. Most are manageable — but your pharmacist should know about everything you take, including vitamins and herbals.

Severity mix
  • Major · 8
  • Moderate · 98
  • Minor · 40
Every supplement checked against Fostemsavir — ranked by severity The full interaction hub: 8 major · 98 moderate · 40 minor · every one linked to its full report. Check Fostemsavir against your exact supplements

Educational information from a licensed clinical database (Natural Medicines) — see our data sources & update cadence. Not medical advice: an interaction being documented does not mean it will happen to you; do not start or stop medications or supplements without professional guidance.

🩺 Pharmacist Counseling Corner

Quick, plain-English answers to the questions patients ask most about Fostemsavir — the kind of thing our pharmacy team would talk through with you at the counter.

Why am I being prescribed Rukobia instead of one of the more common HIV medications? ▾
Rukobia is designed for people who have been on HIV treatment for a long time and whose virus has become resistant to many other drugs — or who couldn't tolerate those other options. It works in a completely different way from most HIV medicines, by blocking the virus before it can even enter your immune cells. That makes it a valuable option when other treatments have stopped working. You're always going to take it alongside at least one or two other HIV medicines, not on its own.
Can I take Rukobia with or without food? ▾
Yes, you can take it either way — with or without food. That said, a very high-fat meal can noticeably increase the amount of medicine that gets into your bloodstream, so try to be consistent in how you take it day to day. The most important thing is to take it twice daily as prescribed, swallowing the tablets whole. Don't crush, chew, or split them.
What side effects should I watch out for? ▾
The most common side effect is nausea, reported in about 1 in 10 people. You might also notice diarrhea, headache, stomach discomfort, fatigue, or rash. Most of these are mild to moderate. The more serious things to call your doctor about are signs of liver trouble (yellowing of your skin or eyes, dark urine), a new or suddenly worse infection or inflammation after you start therapy, or any irregular heartbeat or dizziness. Don't ignore those — reach out quickly.
Are there any medicines I absolutely cannot take with Rukobia? ▾
Yes — a handful of drugs are outright contraindicated because they dramatically lower Rukobia's levels in your blood, which could cause your HIV to become undetectable in terms of treatment response — essentially making the medicine stop working. These include rifampin (a tuberculosis drug), the seizure medicines carbamazepine and phenytoin, the prostate cancer drug enzalutamide, mitotane, and St. John's wort herbal supplement. Make sure every provider you see knows you're on Rukobia before prescribing anything new.
Is it safe to take Rukobia if I'm pregnant or planning to get pregnant? ▾
The honest answer is that we don't have enough human data yet to be certain. Animal studies didn't show harm at typical human exposure levels, but did show problems at very high doses. If you're pregnant or planning to become pregnant, this is definitely a conversation to have with your prescriber right away. There's also a pregnancy registry to help track outcomes — your doctor can enroll you, or you can call 1-800-258-4263 yourself.
I also have hepatitis C — is there anything special I need to know? ▾
Yes, this is important. If you have hepatitis B or C along with HIV, Rukobia can cause your liver enzymes to rise more than it would in someone without a co-infection. Your doctor should monitor your liver tests regularly. Also, if you're on a hepatitis C treatment that contains grazoprevir or voxilaprevir, Rukobia can raise the levels of those drugs and increase your risk of liver enzyme problems — your provider may want to switch you to a different hepatitis C regimen.
Is Fostemsavir available over the counter? ▾
Fostemsavir is dispensed by prescription according to its FDA labeling, so it isn't sold over the counter. Your prescriber and pharmacist will determine if it's appropriate for you.
When was Fostemsavir first available? ▾
Fostemsavir has been available in the United States since at least 2020, based on FDA approval history (Drugs@FDA) and product marketing records.
Who makes Fostemsavir? ▾
Fostemsavir is supplied by 2 manufacturers listed in the FDA NDC Directory, including ViiV Healthcare Company, Piramal Healthcare UK Limited.

💬 Answers drafted from Fostemsavir’s FDA-approved label information, summarized in plain language with AI, and reviewed by our pharmacy team before publication. Grounded in that labeling — nothing is made up. How we use AI →

🧰 Keep exploring

💊 How Fostemsavir comes

Fostemsavir is available in 1 form. Different forms and brands can have different approved uses, doses, schedules, and directions. Follow the instructions for your exact product, and do not switch forms without guidance from your prescriber or pharmacist.

Extended-release tablet

By mouth
Brands Rukobia
How this form is used
What it may be used for
  • Rukobia is used in combination with other antiretrovirals to treat HIV-1 infection in heavily treatment-experienced adults with multidrug-resistant HIV-1 who are failing their current regimen due to resistance, intolerance, or safety concerns
Important instructions
  • Rukobia tablets are taken by mouth twice daily
  • Rukobia can be taken with or without food
  • Swallow Rukobia tablets whole — do not chew, crush, or split them
  • Follow your prescriber's instructions for the full dosing schedule
Available strengths 1 strength
3 FDA-listed product records ⓘ

📊 Fostemsavir across the U.S. market

How Fostemsavir appears in the FDA’s National Drug Code Directory — including its dosage forms, strengths, brand names, manufacturers, and FDA-listed product records. These are directory records, not sales or prescription volume.

1
Dose forms ⓘ
2
Manufacturers
1
Brand names
4
FDA-listed product records ⓘ
2020
First marketed ⓘ

Also listed with the FDA, not a patient dose form: Powder (1) — bulk drug substance sold to compounders/manufacturers and multi-item kits. These aren’t counted in the dose-form total above.

ViiV Healthcare Company75%
Piramal Healthcare UK Limited25%

Share of FDA-listed product records by manufacturer — FDA National Drug Code Directory. Record counts are not sales or prescription volume.

📈 How widely Fostemsavir is used

A general measure of how commonly Fostemsavir is prescribed, based on Medicaid — one of the largest public drug programs. The figure below is prescriptions filled in Q1–Q4 2025, summed across every form and brand of the drug.

Think of this as a proxy for how widely Fostemsavir is used, drawn from freely available public data. Medicaid is just one program — these numbers don’t include Medicare, other government coverage, or commercial and cash-pay prescriptions, so real-world use is higher than what’s shown here.

2,430
Medicaid prescriptions filled (Q1–Q4 2025)
$22.3M gross Medicaid reimbursement (before mandatory rebates — net cost is lower)

How commonly is Fostemsavir prescribed? Of the 1,597 medications we measure, Fostemsavir ranks #1,164 by Medicaid prescriptions — more than 27% of them.

Where Fostemsavir ranks among the drugs we measure · Q1–Q4 2025 · neighbors ±5

Utilization by Fostemsavir product

Pick a product to see its own Medicaid numbers. Each chip is one clinical product — a specific strength & dosage form as defined by RxNorm — with brand-name and generic versions combined.

12 HR fostemsavir 600 MG Extended Release Oral Tablet

2,430 Medicaid prescriptions (Q1–Q4 2025) 100% of Fostemsavir prescriptions shown $22.3M gross reimbursement (before rebates) ≈ $9,176 per prescription (gross)

Summed across the 1 of 1 listed NDC products with Medicaid activity — every brand and generic of this exact strength & form. RxNorm 2380549

Shares are of the Medicaid prescriptions shown here. Product grouping follows RxNorm (the National Library of Medicine’s drug terminology), so “one product” means one strength & dosage form regardless of manufacturer. Dollar figures are gross Medicaid reimbursement before mandatory rebates — rebates (often large, especially for brand-name drugs) are confidential, so actual net cost to Medicaid is lower than shown.

Source: Medicaid State Drug Utilization Data (CMS), aggregated by generic ingredient — summed across every NDC (all brands, strengths, salt forms and dosage forms) of Fostemsavir, and across all states and both fee-for-service and managed-care claims. A general popularity signal; it excludes Medicare, commercial insurance and cash prescriptions, so it is not total U.S. use. Based on the 1 of 1 listed Fostemsavir NDCs with Medicaid activity.

🔍 Compare Fostemsavir products

A representative set of FDA-listed product records for Fostemsavir — across manufacturers, strengths, and dosage forms, grouped by form with each product’s manufacturer and how the FDA approved it. The same medicine may be made and packaged by different companies, so a single drug can have many directory entries. (It’s also why a refill can look different — a new shape, color, or box — even though it contains the same medication.)

Strength Route Manufacturer / Labeler Category ⓘ Details
💊Extended-release tablet
600 mg Oral ViiV Healthcare Company × 3 listings NDA View NDC →
💊Bulk drug substance
15 kg/15 kg — Piramal Healthcare UK Limited BULK INGREDIENT View NDC →

Showing 4 of 4 products — FDA National Drug Code Directory. See every product, package size and price: browse all 4 Fostemsavir NDCs →

RxNorm Concept Web — From Ingredient to Every Form and Strength

This page starts with one ingredient concept (IN). The branches below show its dose-form concepts (SCDF), then the available clinical drug and strength concepts (SCD). Combination products remain separate concepts with their own pages.

Ingredient (IN) Fostemsavir RxCUI 2380373 1 dose form · 1 strength
  1. Dose form (SCDF) Extended Release Oral Tablet RxCUI 2380538 In current FDA listings
    Clinical drug / strength (SCD) 12 HR fostemsavir 600 MG RxCUI 2380549

Look up RxCUI 2380373 in the RxCUI Atlas →

RxNorm is the U.S. National Library of Medicine’s normalized drug vocabulary. Its concept hierarchy can include forms that are not currently marketed; the status on each branch compares that concept with current FDA listings. RxCUIs identify vocabulary concepts, not individual packages or manufacturers.

🏷️ Sold under these brand names

Rukobia

🏭 Manufacturers & labelers

ViiV Healthcare Company 3 Piramal Healthcare UK Limited 1

RxNorm drug class

Fostemsavir belongs to the Other antivirals class.

Drug family (ATC) Other antivirals

Classified by RxNorm RxClass — the U.S. National Library of Medicine's standardized drug-classification service (Established Pharmacologic Class from the FDA, the ATC drug family from the WHO, and mechanism of action). Reference only, not medical advice.

🔬 Where this comes from

Core label, product, RxNorm, safety, and utilization data on this page come from the sources identified below. AI-written, editorial, and licensed sections are labeled separately.

📄
FDA-filed drug labels (SPL) Uses, dosing, warnings & side effects from SPL records retrieved through openFDA; the linked representative set can be verified on DailyMed. ✓ Linked label effective Feb 13, 2024
🏭
Forms, brands & labelersAggregated from ingredient-matched FDA National Drug Code Directory product records for Fostemsavir.
📈
Real-world reportsThe FDA Adverse Event Reporting System (FAERS), served through openFDA.
🚨
Recalls & shortagesopenFDA drug-enforcement reports and the FDA drug-shortage database.
🧾 Clinical label set — FDA-filed SPL labels retained for Fostemsavir after exact ingredient or ingredient-combination matching and applicable route/form matching
Clinical labels in scope
1
NDC products indexed
4
Distinct labelers/manufacturers represented
2
Linked representative label ⓘ
ViiV Healthcare Company
Linked label effective
Feb 13, 2024
Composite sections available
21
Linked SPL Set ID
a21006b7-6d6f-4f06-81b4-17978756452b
Linked SPL Document ID
6c5f162a-40d2-4024-badd-6e80ec4641d7
Open the linked representative label on DailyMed ↗

How we combine label and product data

HelloPharmacist combines public FDA and NLM records; we don’t author the underlying clinical facts. We identified 1 FDA-filed SPL label set within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. The representative label is the starting point for the displayed reference monograph; the 12 largest stored in-scope SPL records, which may include that representative, are compared section by section, and the longest available version of each section is retained. Forms, routes, brands, labelers, product-listed strengths, and product-record counts are aggregated separately from ingredient-matched FDA NDC Directory records; package records listed above are associated with the linked SPL; and the normalized concept hierarchy comes from NLM RxNorm.

For canonical ingredient pages, bounded product-attributed indication and administration excerpts may be added to the AI evidence, and the generator is instructed to preserve available product, brand, route, and form qualifiers instead of treating one label as universal. Where a section is identified as AI-written, its plain-language text is generated from bounded label evidence. New draft drug pages remain in the admin review queue before first publication. ViiV Healthcare Company is the representative DailyMed label linked for verification and dates; it is not the sole source used for the page.

This is general education, not medical advice — always consult your doctor or pharmacist about your medications and any medical condition. For the exact wording of the linked representative label, view that label on DailyMed; some displayed composite sections may come from other in-scope SPL labels. Learn how we use AI and our data sources & update cadence.