Fostemsavir tromethamine

What is Fostemsavir tromethamine?

Fostemsavir tromethamine (RUKOBIA), a human immunodeficiency virus type 1 (HIV-1) gp120-directed attachment inhibitor a prescription medicine that is used with other antiretroviral medicines to treat Human Immunodeficiency Virus (HIV-1) infection in adults.

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What are the uses of this medicine?

This medicine is is used with other antiretroviral medicines to treat Human Immunodeficiency Virus (HIV-1) infection in adults who:

• have received several anti-HIV-1 regimens in the past, and
• have HIV-1 virus that is resistant to many antiretroviral medicines, and
• are failing their current antiretroviral therapy. You could be failing therapy because it is not working or no longer works, you are not able to tolerate the side effects, or there are other safety reasons why you cannot take it.

HIV-1 is the virus that causes Acquired Immune Deficiency Syndrome (AIDS).

How does this medicine work?

• Fostemsavir is an HIV-1 antiretroviral agent.
• Fostemsavir is a prodrug without significant biochemical or antiviral activity that is hydrolyzed to the active moiety, temsavir, which is an HIV-1 attachment inhibitor.
• Temsavir binds directly to the gp120 subunit within the HIV-1 envelope glycoprotein gp160 and selectively inhibits the interaction between the virus and cellular CD4 receptors, thereby preventing attachment.
• Additionally, temsavir can inhibit gp120-dependent post-attachment steps required for viral entry into host cells.
• Temsavir inhibited the binding of soluble CD4 to surface immobilized gp120 with an IC50 value of 14 nM using an enzyme-linked immunosorbent assay (ELISA).

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• with previous hypersensitivity to fostemsavir or any of the components of RUKOBIA.

What drug interactions can this medicine cause?

This medicine cannot be coadministered with 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

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

Is this medicine FDA approved?

• It was approved for use in the United States in 2020.

How should this medicine be used?

• The recommended dosage of RUKOBIA is one 600-mg tablet taken orally twice daily with or without food.

Administration

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

This medicine is available in fallowing doasage form: As extended-release tablets: 600 mg

This medicine is available in fallowing brand namesː

• RUKOBIA

What side effects can this medication cause?

Common possible side effects of this medicine include:

• nausea

This medicine can cause serious side effects including:

• Changes in your immune system (Immune Reconstitution Syndrome)
• Heart rhythm problems (QTc prolongation)
• Changes in liver function blood tests results

What special precautions should I follow?

• Fatal and serious myelosuppression and infectious complications may occur. Obtain complete blood cell counts prior to initiation of INQOVI, prior to each cycle, and as clinically indicated to monitor for response and toxicity.
• Delay the next cycle and resume at the same or reduced dose as recommended.
• Advise patients of reproductive potential of the potential risk to a fetus and to use effective contraception.

What to do in case of emergency/overdose?

• 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.

Can this medicine be used in pregnancy?

• There are insufficient human data on the use of RUKOBIA during pregnancy to adequately assess a drug-associated risk of birth defects and miscarriage.
• 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.

Can this medicine be used in children?

• The safety and effectiveness of RUKOBIA have not been established in pediatric patients.

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.

• Dailymed label info on Fostemsavir tromethamine
• FDA Fostemsavir tromethamine

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