Fostemsavir

RUKOBIA is an HIV-1 antiretroviral agent [see Microbiology ( 12.4 )].

• RUKOBIA, in combination with other antiretroviral(s), is indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in heavily treatment-experienced adults with multidrug-resistant HIV-1 infection failing their current antiretroviral regimen due to resistance, intolerance, or safety considerations [see Clinical Studies ( 14 )]. RUKOBIA, a human immunodeficiency virus type 1 (HIV-1) gp120-directed attachment inhibitor, in combination with other antiretroviral(s), is indicated for the treatment of HIV-1 infection in heavily treatment-experienced adults with multidrug-resistant HIV-1 infection failing their current antiretroviral regimen due to resistance, intolerance, or safety considerations.ICD-10: B20

• RUKOBIA is contraindicated in patients: • with previous hypersensitivity to fostemsavir or any of the components of RUKOBIA. • coadministered strong cytochrome P450 (CYP)3A inducers, as significant decreases in temsavir (the active moiety of fostemsavir) plasma concentrations may occur which may result in loss of virologic response.contraindicated

The recommended dosage of RUKOBIA is one 600-mg tablet taken orally twice daily with or without food [see Clinical Pharmacology ( 12.3 )] . Swallow tablets whole. Do not chew, crush, or split tablets. One tablet taken twice daily with or without food. ( 2 )

• Immune reconstitution syndrome has been reported in patients treated with combination antiretroviral therapies. ( 5.1 ) • QTc prolongation: Use RUKOBIA with caution in patients with a history of QTc prolongation or with relevant pre-existing cardiac disease or who are taking drugs with a known risk of Torsade de Pointes. ( 5.2 ) • Elevations in hepatic transaminases in patients with hepatitis B (HBV) or C (HCV) virus co-infection: Elevations in hepatic transaminases were observed in a greater proportion of subjects with HBV and/or HCV co-infection compared with those with HIV mono-infection. ( 5.3 ) 5.1 Immune Reconstitution Syndrome Immune reconstitution syndrome has been reported in patients treated with combination antiretroviral therapy, including RUKOBIA [see Adverse Reactions ( 6.1 )] . During the initial phase of combination antiretroviral treatment, patients whose immune systems respond may develop an inflammatory response to indolent or residual opportunistic infections (such as Mycobacterium avium infection, cytomegalovirus, Pneumocystis jirovecii pneumonia [PCP], or tuberculosis), which may necessitate further evaluation and treatment. Autoimmune disorders (such as Graves’ disease, polymyositis, Guillain-Barré syndrome, and autoimmune hepatitis) have also been reported to occur in the setting of immune reconstitution; however, the time to onset is more variable and can occur many months after initiation of treatment.

The following adverse reactions are discussed in greater detail in other sections of the labeling: • Immune reconstitution syndrome [see Warnings and Precautions ( 5.1 )] . • QTc prolongation [see Warnings and Precautions ( 5.2 )] . • Elevations in hepatic transaminases in patients with hepatitis B or C virus co-infection [see Warnings and Precautions ( 5.3 )]. The most common adverse reaction (all grades) observed in ≥5% of subjects was nausea. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact ViiV Healthcare at 1-877-844-8872 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical 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 with rates in the clinical trials of another drug and may not reflect the rates observed in practice. A total of 620 subjects with HIV-1 infection received at least one dose of RUKOBIA as part of a controlled clinical trial. The primary safety assessment of RUKOBIA is based on 96 weeks of data from a Phase 3 partially randomized, international, multicenter, double-blind, placebo-controlled trial (BRIGHTE) conducted in 371 heavily treatment-experienced adult subjects [see Clinical Studies ( 14 )] . In the randomized cohort, 203 subjects received at least one dose of blinded RUKOBIA 600 mg twice daily and 69 subjects received placebo in addition to their current failing regimen for 8 days of functional monotherapy.

8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in individuals exposed to RUKOBIA during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary There are insufficient human data on the use of RUKOBIA during pregnancy to adequately assess a drug-associated risk of birth defects and miscarriage. In animal reproduction studies, oral administration of fostemsavir to pregnant rats and rabbits during organogenesis resulted in no adverse developmental effects at clinically relevant temsavir exposures (see Data) . The background risk for major birth defects and miscarriage for the indicated population is unknown. The background rate for major birth defects in a U.S. reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP) is 2.7%. The estimated background rate of miscarriage in clinically recognized pregnancies in the U.S. general population is 15% to 20%. Data Animal Data: Fostemsavir was administered orally to pregnant rats (50, 200, 600 mg/kg/day) and rabbits (25, 50, or 100 mg/kg/day) during Gestation Days 6 to 15 (rat) and 7 to 19 (rabbit).

Metabolism

Fostemsavir is a prodrug of temsavir, its active moiety. Fostemsavir was generally not detectable in plasma following oral administration.

There is no known specific treatment for overdose with RUKOBIA. If overdose occurs, the patient should be monitored and standard supportive treatment applied as required, including monitoring of vital signs and ECG (QT interval), as well as observation of the clinical status of the patient. As fostemsavir is highly bound to plasma proteins, it is unlikely that it will be significantly removed by dialysis.

• Jul 2, 2020NDANDA212950Viiv Hlthcare

1. 1Off Label Use2913%
2. 2Nausea177.5%
3. 3Death156.6%
4. 4Product Dose Omission Issue156.6%
5. 5Drug Ineffective146.2%
6. 6Rash114.8%
7. 7Viral Load Increased114.8%
8. 8Dizziness94.0%
9. 9Fatigue94.0%
10. 10Pathogen Resistance94.0%
11. 11Product Residue Present94.0%
12. 12Virologic Failure94.0%
13. 13Wrong Technique In Product Usage Process94.0%
14. 14Diarrhoea73.1%
15. 15Dysphagia73.1%

The 10 most recently updated of 25 ClinicalTrials.gov registrations naming Fostemsavir as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study to Investigate the Use of VH3810109 With or Without Fostemsavir (FTR) to Reduce the Size and Activity of the Viral Reservoir in People Living With HIV
  Active not recruiting · Phase 1 · Interventional · 107 enrolled · ViiV Healthcare
  NCT07053384updated 2026-03-24
• Safety and Pharmacokinetics Evaluation of Fostemsavir + (OBT) in HIV-1 Infected Children and Adolescents Who Are Failing Their cART and Have Dual- or Triple-class Antiretroviral Resistance
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 60 enrolled · PENTA Foundation
  NCT04648280updated 2026-03-05
• A Continued Access Study for Participants Transitioning From ViiV Healthcare-sponsored or ViiV Healthcare-collaborative Parent Studies for HIV Treatment
  Not yet recruiting · Phase 3 · Interventional · 183 enrolled · ViiV Healthcare
  NCT07393659updated 2026-02-06
• Reducing Systemic Inflammation in People on Antiretroviral Therapy
  Recruiting · Phase 2 · Interventional · 150 enrolled · Centre hospitalier de l'Université de Montréal (CHUM)
  NCT07030920updated 2025-11-19
• Study to Compare Bictegravir/Lenacapavir Versus Current Therapy in People With HIV-1 Who Are Successfully Treated With a Complicated Regimen
  Active not recruiting · Phase 2 · Phase 3 · Interventional · 689 enrolled · Gilead Sciences
  NCT05502341updated 2025-10-14
• Attachment Inhibitor Comparison in Heavily Treatment Experienced Patients
  Active not recruiting · Phase 3 · Interventional · 371 enrolled · ViiV Healthcare
  NCT02362503updated 2025-08-22
• Changes in Immunologic Parameters Following the Addition of Fostemsavir in Virologically Suppressed Immunologic Non-responders Living With HIV-the RECOVER Study
  Active not recruiting · Phase 4 · Interventional · 25 enrolled · Orlando Immunology Center
  NCT05220358updated 2025-08-03
• Fostemsavir Compassionate Use Named Patient Program for the Treatment of Human Immunodeficiency Virus 1 (HIV-1)
  Available · Expanded access · ViiV Healthcare
  NCT04233047updated 2025-05-13
• Low-dose Fostemsavir Extended Release Relative Bioavailability Study
  Completed · Phase 1 · Interventional · 32 enrolled · ViiV Healthcare
  NCT04757974updated 2021-09-22
• Pharmacodynamics, Safety and Pharmacokinetics of BMS-663068, an HIV Attachment Inhibitor, in HIV-1
  Completed · Phase 2 · Interventional · 50 enrolled · ViiV Healthcare
  NCT01009814updated 2020-01-03

Frequently asked questions

How does Fostemsavir work?

RUKOBIA is an HIV-1 antiretroviral agent [see Microbiology ( 12.4 )].

What is Fostemsavir used for?

According to FDA labeling, Fostemsavir carries indications including: RUKOBIA, in combination with other antiretroviral(s), is indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in heavily treatment-experienced adults with multidrug-resistant HIV-1 infection failing their current antiretroviral regimen due to resistance, intolerance, or safety considerations [see Clinical Studies ( 14 )]. RUKOBIA, a human immunodeficiency virus type 1 (HIV-1) gp120-directed attachment inhibitor, in combination with other antiretroviral(s), is indicated for the treatment of HIV-1 infection in heavily treatment-experienced adults with multidrug-resistant HIV-1 infection failing their current antiretroviral regimen due to resistance, intolerance, or safety considerations.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Fostemsavir?

Fostemsavir is classified as Other antivirals, Cytochrome P450 3A Inducers, HIV 1 Post-attachment Fusion Inhibitors.

What are the brand names for Fostemsavir?

Fostemsavir is marketed under brand names including Rukobia.

What are the contraindications for Fostemsavir?

Fostemsavir labeling lists contraindications including: RUKOBIA is contraindicated in patients: • with previous hypersensitivity to fostemsavir or any of the components of RUKOBIA. • coadministered strong cytochrome P450 (CYP)3A inducers, as significant decreases in temsavir (the active moiety of fostemsavir) plasma concentrations may occur which may result in loss of virologic response.. Always consult the full prescribing information and a clinician.