Fostemsavir

Fostemsavir Brand Name– Rukobia

What is Fostemsavir

Fostemsavir is indicated for use in combination with other antiretroviral agents to treat heavily treatment-experienced adults with multidrug-resistant HIV-1 infections who are failing their current antiretroviral regimen due to resistance, intolerance, or safety considerations.

Fostemsavir is the first approved HIV-1 attachment inhibitor, which works by binding to the glycoprotein 120 (gp120) subunit within the HIV-1 envelope and selectively inhibiting the interaction between the virus and cellular CD4 receptors.

Health care providers are advised to consider potential drug interactions prior to and during treatment with fostemsavir because the drug is partially metabolized by CYP3A4 and supratherapeutic doses have been associated with prolongation of the QT interval.

Indications

  • human immunodeficiency virus (HIV)
  • human immunodeficiency virus (HIV) infection

Side Effects

  1. abdominal pain
  2. abnormal dreams
  3. anemia
  4. asthenia
  5. diarrhea
  6. dizziness
  7. drowsiness
  8. dysgeusia
  9. dyspepsia
  10. elevated hepatic enzymes
  11. fatigue
  12. headache
  13. hyperbilirubinemia
  14. hypercholesterolemia
  15. hyperglycemia
  16. hypertriglyceridemia
  17. insomnia
  18. maculopapular rash
  19. myalgia
  20. nausea
  21. neutropenia
  22. peripheral neuropathy
  23. pruritus
  24. QT prolongation
  25. rash
  26. vomiting

Monitoring Parameters

  • blood glucose
  • CBC with differential
  • CD4+ T cell count
  • hepatitis B serology
  • LFTs
  • plasma hepatitis C RNA
  • plasma HIV RNA
  • pregnancy testing
  • serum bilirubin (total and direct)
  • serum cholesterol
  • serum lipid profile
  • urinalysis

Contraindications

  • apheresis
  • autoimmune disease
  • AV block
  • bradycardia
  • breast-feeding
  • cardiomyopathy
  • celiac disease
  • females
  • fever
  • geriatric
  • Graves’ disease
  • Guillain-Barre syndrome
  • heart failure
  • hepatitis B and HIV coinfection
  • hepatitis C and HIV coinfection
  • human immunodeficiency virus (HIV) infection resistance
  • hyperparathyroidism
  • hypocalcemia
  • hypokalemia
  • hypomagnesemia
  • hypothermia
  • hypothyroidism
  • immune reconstitution syndrome
  • long QT syndrome
  • myocardial infarction
  • pheochromocytoma
  • pregnancy
  • QT prolongation
  • rheumatoid arthritis
  • sickle cell disease
  • sleep deprivation
  • stroke
  • systemic lupus erythematosus (SLE)

Interactions

  • Abacavir; Dolutegravir; Lamivudine
  • Alpelisib
  • Amlodipine; Atorvastatin
  • Apalutamide
  • Aspirin, ASA; Pravastatin
  • Atorvastatin
  • Atorvastatin; Ezetimibe
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Bictegravir; Emtricitabine; Tenofovir Alafenamide
  • Bosentan
  • Carbamazepine
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Dolutegravir
  • Dolutegravir; Lamivudine
  • Dolutegravir; Rilpivirine
  • Drospirenone; Ethinyl Estradiol
  • Drospirenone; Ethinyl Estradiol; Levomefolate
  • Elagolix
  • Elagolix; Estradiol; Norethindrone acetate
  • Elbasvir; Grazoprevir
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Emtricitabine; Rilpivirine; Tenofovir alafenamide
  • Emtricitabine; Tenofovir alafenamide
  • Enzalutamide
  • Ethinyl Estradiol
  • Ethinyl Estradiol; Desogestrel
  • Ethinyl Estradiol; Ethynodiol Diacetate
  • Ethinyl Estradiol; Etonogestrel
  • Ethinyl Estradiol; Levonorgestrel
  • Ethinyl Estradiol; Levonorgestrel; Ferrous bisglycinate
  • Ethinyl Estradiol; Levonorgestrel; Folic Acid; Levomefolate
  • Ethinyl Estradiol; Norelgestromin
  • Ethinyl Estradiol; Norethindrone
  • Ethinyl Estradiol; Norethindrone Acetate
  • Ethinyl Estradiol; Norethindrone Acetate; Ferrous fumarate
  • Ethinyl Estradiol; Norethindrone; Ferrous fumarate
  • Ethinyl Estradiol; Norgestimate
  • Ethinyl Estradiol; Norgestrel
  • Ezetimibe; Simvastatin
  • Fluvastatin
  • Fosphenytoin
  • Glecaprevir; Pibrentasvir
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Letermovir
  • Lovastatin
  • Lovastatin; Niacin
  • Mitotane
  • Niacin; Simvastatin
  • Ombitasvir; Paritaprevir; Ritonavir
  • Ozanimod
  • Pazopanib
  • Phenobarbital
  • Phenytoin
  • Pitavastatin
  • Pravastatin
  • Primidone
  • Revefenacin
  • Rifampin
  • Rifapentine
  • Rimegepant
  • Rosuvastatin
  • Segesterone Acetate; Ethinyl Estradiol
  • Simvastatin
  • Simvastatin; Sitagliptin
  • Sofosbuvir; Velpatasvir; Voxilaprevir
  • St. John’s Wort, Hypericum perforatum
  • Talazoparib
  • Tenofovir Alafenamide
  • Tenofovir Alafenamide
  • Topotecan
  • Ubrogepant
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