How Far Is Too Far? The Ethics of Mini Brain Research
December 11, 2025
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Brand Name :
Rukobia
Synonyms :
fostemsavir
Class :
Attachment Inhibitor, Antiretroviral agent
Brand Name :
Rukobia
Synonyms :
fostemsavir
Class :
Attachment Inhibitor, Antiretroviral agent
Dosage Forms & Strengths
Extended-release tablet
600mg
Indicated in combination with other antiretroviral (ATV) medications for treating HIV-1 infection:
600mg orally twice a day
Safety and efficacy not established
Refer adult dosing
may decrease the levels of serum concentration of hormonal contraceptives
may decrease the levels of serum concentration of hormonal contraceptives
may decrease the levels of serum concentration of hormonal contraceptives
may decrease the levels of serum concentration of hormonal contraceptives
may enhance the serum concentration of BCRP/ABCG2 inhibitors
may enhance the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors
may enhance the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors
may enhance the serum concentration of BCRP/ABCG2 inhibitors
may enhance the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors
may enhance the serum concentration of fostemsavir
may enhance the serum concentration of fostemsavir
may enhance the serum concentration of fostemsavir
may enhance the serum concentration of fostemsavir
may enhance the serum concentration of fostemsavir
may enhance the serum concentration of BCRP/ABG2 inhibitors
When naficillin combines with fostemsavir, nafcillin will decrease the effect of action of fostemsavir by affecting enzyme CYP3A4 metabolism.
when both drugs are combined, there may be a decreased effect of fostemsavir by affecting hepatic or intestinal enzyme cyp3a4 metabolism
may enhance the serum concentration of HMG-CoA Reductase Inhibitors
may diminish the serum concentration of Hormonal Contraceptives
by altering intestinal/hepatic CYP 3A4 metabolism, the activity of fostemsavir can be reduced by butabarbital
may enhance the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors
may enhance the serum concentration of fostemsavir
may enhance the serum concentration of fostemsavir
may enhance the serum concentration of fostemsavir
may enhance the serum concentration of fostemsavir
may enhance the serum concentration of fostemsavir
may enhance the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors
may enhance the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors
may enhance the serum concentration of BCRP/ABG2 inhibitors
may enhance the serum concentration of P-glycoprotein/ABCB1 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
the levels of lenvanitib are increased by fostemsavir or vice-versa
CYP3A enhancers (strong) may reduce the plasma concentrations of the active metabolite(s) of fostemsavir
may intensify the potentially negative effects of HMG-CoA Reductase Inhibitors
may enhance the serum concentration
may increase the QTc prolonging effect of QT-prolonging agents
may increase the QTc prolonging effect of QT-prolonging agents
may increase the QTc prolonging effect of QT-prolonging agents
may increase the QTc prolonging effect of QT-prolonging agents
may increase the QTc prolonging effect of QT-prolonging agents
may enhance the serum concentration of BCRP/ABG2 inhibitors
It may enhance the risk of adverse effects when combined with Protease inhibitors
decrease the metabolism of daunorubicin and increase serum levels
when both drugs are combined, both increase the QTC interval
decrease the metabolism of idarubicin and increase serum levels
may increase the serum concentration of Artemether and Lumefantrine
cyproterone and ethinyl estradiol
may diminish the serum concentration when combined
It may enhance the serum concentration when combined with CYP3A4 Substrates
It may enhance the serum concentration when combined with CYP3A4 Substrates
It may enhance the serum concentration when combined with CYP3A4 Substrates
tenofovir disoproxil fumarate or tenofovir DF
monitoring of patients who develop TDF-associated adverse reactions in which tenofovir levels increase when taken along with HIV-1 protease inhibitors. If TDF-associated adverse reactions emerge, discontinue tenofovir DF in patients who develop them
the risk of QTc prolongation may be increased
Actions and Spectrum:
fostemsavir is an antiretroviral medication that belongs to the class of drugs known as attachment inhibitors. It prevents the human immunodeficiency virus (HIV) from binding to the CD4+ receptor on the surface of human immune cells, which is necessary for the virus to enter and infect the cell
The spectrum of activity of fostemsavir is limited to HIV-1, the most common strain of HIV that causes acquired immunodeficiency syndrome (AIDS) in humans.
fostemsavir is indicated for treating HIV-1 infection in heavily treatment-experienced adults with multidrug-resistant HIV-1 who cannot achieve viral suppression with other therapies
Frequency defined
>10%
Creatinine >1.8 x ULN or 1.5 x baseline (19%)
1-10%
Nausea (10%)
Hemoglobin <9 g/dL (6%)
Lipase >3x ULN (5%)
ALT >5x ULN (5%)
Hyperglycemia >250 mg/dL (4%)
Neutrophils ≤599 cells/mm3 (4%)
Headache (4%)
Urate >12 mg/dL (3%)
Dyspepsia (3%)
Rash (3%)
Immune reconstitution inflammatory syndrome (2%)
Vomiting (2%)
Direct bilirubin >ULN (7%)
Cholesterol ≥300 mg/dL) (5%)
Triglycerides >500 mg/dL (5%)
AST >5x ULN (4%)
LDL cholesterol ≥190 mg/dL
Diarrhea (4%)
Bilirubin ≥2.6x ULN (3%)
Abdominal pain (3%)
Fatigue (3%)
Sleep disturbance (3%)
Somnolence (2%)
Creatinine kinase ≥10x ULN (2%)
<2%
Myalgia
Dysgeusia
Pruritis
Peripheral neuropathy
ECG QT Prolonged
Dizziness
Contraindications/caution:
Contraindications:
Caution:
Pregnancy consideration: fostemsavir is not recommended for use during pregnancy, as its safety and efficacy in pregnant women have not been studied
Lactation: Excretion of the drug in human breast milk is unknown
Pregnancy category:
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology:
Pharmacodynamics:
Pharmacokinetics:
Absorption
fostemsavir is administered orally as a prodrug (fostemsavir tromethamine) and is rapidly absorbed from the gastrointestinal tract. Administration of a high-fat meal increases drug exposure compared to fasting. The bioavailability of fostemsavir is approximately 26.9%, and peak plasma concentration is achieved in about 2 hours
Distribution
fostemsavir is highly protein-bound (88.4%), primarily to albumin, and has a volume of distribution (Vd) of 29.5 L
Metabolism
fostemsavir is metabolized in the liver by esterases (36.1%) and CYP3A4 (21.2%) and, to a lesser extent, by UDP-glucuronosyltransferases (UGT) (<1%). The prodrug fostemsavir tromethamine is rapidly converted to the active form, temsavir, which is metabolized by esterases and CYP3A4
Elimination and Excretion
The elimination half-life of fostemsavir is approximately 11 hours, and the drug is primarily eliminated through the kidneys (51%), with less than 2% excreted unchanged in the urine. Fecal elimination accounts for approximately 33% of the total elimination, with 1.1% excreted unchanged in the feces. The clearance of fostemsavir is 17.9 L/hr
Administration:
Patient information leaflet
Generic Name: fostemsavir
Pronounced: [ fos-TEM-sa-vir ]
Why do we use fostemsavir?
fostemsavir is indicated for treating HIV-1 infection in heavily treatment-experienced adults with multidrug-resistant HIV-1 infection who are failing their current antiretroviral regimen
It is combined with other antiretroviral agents to suppress HIV-1 replication and improve immune function in these patients
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