Fostemsavir

What is Fostemsavir?

Fostemsavir (brand name:RUKOBIA), in combination with other antiretroviral(s), is used in the treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults with multidrug-resistant HIV-1 infection failing their current antiretroviral regimen.

What are the uses of this medicine?

Rukobia (fostemsavir), is a new type of antiretroviral medication for adults living with HIV who have tried multiple HIV medications and whose HIV infection cannot be successfully treated with other therapies because of resistance, intolerance or safety considerations.

How does this medicine work?

Fostemsavir is the prodrug of temsavir, an HIV-1 attachment inhibitor.

Who Should Not Use this medicine?

RUKOBIA should not be used 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.

These drugs include, but are not limited to:

• Androgen receptor inhibitor: Enzalutamide
• Anticonvulsants: Carbamazepine, phenytoin
• Antimycobacterial: Rifampin
• Antineoplastic: Mitotane
• Herbal product: St John’s wort (Hypericum perforatum)

Is this medicine FDA approved?

Yes, it is FDA approved on Jul 2, 2020

What are the dosage forms and brand names of this medicine?

Each RUKOBIA extended-release tablet contains 600 mg of fostemsavir (equivalent to 725 mg of fostemsavir tromethamine). The tablets are beige, oval, film-coated, biconvex tablets, debossed with “SV 1V7” on one side. The recommended dosage of RUKOBIA is one 600-mg tablet taken orally twice daily with or without food.

How should this medicine be used?

• Take RUKOBIA exactly as your healthcare provider tells you to take it.
• Take RUKOBIA tablets whole. Do not chew, crush, or split RUKOBIA tablets before swallowing.
• Take RUKOBIA with or without food.
• RUKOBIA tablets may have a slight odor (like vinegar). This is normal.
• Do not miss a dose of RUKOBIA. If you miss a dose of RUKOBIA, take it as soon as you remember. Do not take 2 doses at the same time or take more than your healthcare provider tells you to take.
• Do not run out of RUKOBIA. The virus in your blood may increase and the virus may become harder to treat. When your supply starts to run low, get more from your healthcare provider or pharmacy.
• If you take too much RUKOBIA, call your healthcare provider or go to the nearest hospital emergency room right away.

What side effects can this medication cause?

The most common side effect of RUKOBIA is nausea.

RUKOBIA can cause serious side effects including:

• Changes in your immune system (Immune Reconstitution Syndrome) can happen when you start taking HIV-1 medicines. Your immune system may get stronger and begin to fight infections that have been hidden in your body for a long time. Tell your healthcare provider right away if you start having new symptoms after you start taking RUKOBIA.

• Heart rhythm problems (QTc prolongation). RUKOBIA may cause a heart rhythm problem called QTc prolongation. QTc prolongation causes an irregular heartbeat. If you are elderly, you may be at a greater risk for developing this heart problem with RUKOBIA.

• Tell your healthcare provider right away if you feel dizzy, lightheaded, feel changes in your heartbeat, or you faint (lose consciousness).

• Changes in liver function blood tests results. People with HIV-1 who take RUKOBIA and who also have hepatitis B or C virus infections, may be more likely to develop new or worsening changes in certain liver function blood tests during treatment with RUKOBIA.

• If you stop your anti-hepatitis B treatment, this could mean that your hepatitis B may become active again (reactivated). Your healthcare provider may do blood tests to check your liver during treatment with RUKOBIA especially if you have hepatitis B virus infection.

• Take any anti-hepatitis B or anti-hepatitis C medicines as prescribed by your healthcare provider during treatment with RUKOBIA.

Immune Reconstitution Syndrome

Immune reconstitution syndrome has been reported in patients treated with combination antiretroviral therapy, including RUKOBIA 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.

QTc Prolongation with Higher than Recommended Dosages

RUKOBIA at 2,400 mg twice daily, 4 times the recommended daily dose, has been shown to significantly prolong the QTc interval of the electrocardiogram

Elevations in Hepatic Transaminases in Patients with Hepatitis B or C Virus Co-infection

Monitoring of liver chemistries is recommended in patients with hepatitis B and/or C 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.

Risk of Adverse Reactions or Loss of Virologic Response Due to Drug Interactions

The concomitant use of RUKOBIA and certain other drugs may result in known or potentially significant drug interactions leading to:

• Loss of therapeutic effect of RUKOBIA and possible development of resistance due to reduced exposure of temsavir.
• Possible prolongation of QTc interval from increased exposure to temsavir .

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

No

Can this medicine be used in children?

No

What should I know about storage and disposal of this medication?

• Store RUKOBIA at room temperature between 68°F to 77°F (20°C to 25°C).
• RUKOBIA comes in a child-resistant package.

What are the ingredients in RUKOBIA?

Active ingredient: fostemsavir.

Inactive ingredients: colloidal silicon dioxide, hydroxypropyl cellulose, hypromellose, and magnesium stearate.

The tablet film-coating contains: iron oxide red, iron oxide yellow, polyethylene glycol, polyvinyl alcohol, talc, and titanium dioxide.

• Dailymed label info on Fostemsavir
• FDA Fostemsavir

Fostemsavir Resources
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