Tenofovir alafenamide

VEMLIDY

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FDA label

BOXED WARNING Severe acute HBV exacerbations reported after discontinuation in individuals with HBV — monitor hepatic function closely for several months after stopping; anti-HBV therapy may be warranted. For HIV-1 PrEP: prescribe only to individuals confirmed HIV-negative immediately before initiation and at least every 3 months during use — drug-resistant HIV-1 variants have emerged when PrEP was used during undetected acute HIV-1 infection.

FDA dosing	Population	Start	Target	Max
HIV-1 treatment (with other antiretrovirals)	Adults & peds ≥35 kg	1 tab (FTC 200 mg/TAF 25 mg) QD	200/25 mg QD	1 tab QD
HIV-1 treatment (with other ARVs incl. DRV+COBI, but not other PIs boosted with ritonavir or cobicistat)	Peds 25 to <35 kg	1 tab (200/25 mg) QD	200/25 mg QD	1 tab QD
HIV-1 treatment (same ARV restriction as above)	Peds 14 to <25 kg	1 tab (FTC 120 mg/TAF 15 mg) QD	120/15 mg QD	1 tab QD
HIV-1 PrEP (individuals at risk, excluding risk from receptive vaginal sex)	Adults & adolescents ≥35 kg, HIV-negative	1 tab (200/25 mg) QD	200/25 mg QD	1 tab QD

Renal CrCl ≥30: no adjustment. CrCl 15-<30, or <15 not on hemodialysis: not recommended. Adults with ESRD (CrCl <15) on chronic hemodialysis: no adjustment — dose after hemodialysis on dialysis days

Hepatic Mild-moderate (Child-Pugh A/B): no adjustment; severe (C): not studied

Fixed-dose combination with emtricitabine; Descovy alone is not a complete HIV-1 treatment regimen

Instructions

With or without food
Test for HBV before or when initiating
Assess serum creatinine, estimated CrCl, urine glucose and urine protein before/when initiating and during use; add serum phosphorus if chronic kidney disease
PrEP: confirm HIV-negative immediately prior to start and at least every 3 months and after any STI diagnosis; use an acute-infection assay if recent (<1 mo) exposure or acute HIV symptoms; counsel on daily adherence and safer sex

Contraindications

For HIV-1 PrEP: unknown or positive HIV-1 status

Cautions

Severe acute HBV exacerbation on discontinuation in HBV-coinfected individuals — monitor months after stopping
PrEP: risk of HIV-1 resistance if used during undiagnosed HIV-1 infection; adherence strongly correlated with efficacy
New or worsening renal impairment (acute renal failure, proximal tubulopathy, Fanconi syndrome reported) — avoid with nephrotoxic agents; discontinue for significant renal decline
Lactic acidosis/severe hepatomegaly with steatosis, including fatal cases — suspend if suspected
Immune reconstitution syndrome (treatment)

Adverse reactions

HIV-1 treatment: nausea (≥10%)
PrEP (DISCOVER): diarrhea (5%), nausea, headache, fatigue, abdominal pain
Lipid increases (total cholesterol, LDL, triglycerides); small BMD and renal laboratory changes
Postmarketing (TAF products): renal impairment incl. acute renal failure, proximal renal tubulopathy, Fanconi syndrome

Pregnancy Antiretroviral Pregnancy Registry: no statistically significant increase in overall major birth defects for FTC or TAF vs background (2.7%); pregnancy registry available (1-800-258-4263)

Lactation FTC, TAF, and tenofovir present in human milk; no adverse effects reported in breastfed children; risks include HIV-1 transmission to uninfected infants and viral resistance in infected infants

NO BOXED WARNINGS

Classes and tags

Clinical profile

Direct muscarinic antagonism0 / 4

Mechanism of action: Tenofovir alafenamide ballicule

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