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Yeztugo
lenacapavir
Black Box Warnings .
Drug Resistance Risk in Undiagnosed HIV-1 Infection
test patients for HIV-1 infection prior to starting lenacapavir and with each subsequent injection; drug-resistant variants identified in patients with undiagnosed HIV-1 infection; do not start lenacapavir unless negative HIV-1 infection status confirmed; patients infected with HIV-1 must transition to a complete tx regimen
Adult Dosing .
Dosage forms: TAB: 300 mg; INJ: various
HIV pre-exposure prophylaxis
- [>35 kg]
- Dose: 927 mg SC q6mo; Start: 927 mg SC x1 and 600 mg PO x1 on Day 1, then 600 mg PO x1 on Day 2; Info: may give injection up to 2wk before or after scheduled dose; check HIV status with HIV-1 RNA before tx start and with every injection or upon diagnosis of other sexually transmitted infections; see pkg insert for missed dose recommendations
renal dosing
- [see below]
- CrCl >15: no adjustment; CrCl <15: not defined
- HD/PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class A or B: no adjustment; Child-Pugh Class C: not defined
Peds Dosing .
- Dosage forms: TAB: 300 mg; INJ: various
HIV pre-exposure prophylaxis
- [adolescents, >35 kg]
- Dose: 927 mg SC q6mo; Start: 927 mg SC x1 and 600 mg PO x1 on Day 1, then 600 mg PO x1 on Day 2; Info: may give injection up to 2wk before or after scheduled dose; check HIV status with HIV-1 RNA before tx start and with every injection or upon diagnosis of other sexually transmitted infections; see pkg insert for missed dose recommendations
renal dosing
- [see below]
- CrCl >15: no adjustment; CrCl <15: not defined
- HD/PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class A or B: no adjustment; Child-Pugh Class C: not defined
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- HIV status, positive or unknown (HIV pre-exposure prophylaxis use)
- avoid: breastfeeding (HIV infection use in patients with non-virological suppression throughout 3rd trimester)
- avoid: breastfeeding (HIV infection use in patients with non-virological suppression postpartum)
- avoid: breastfeeding (HIV infection use in patients with cracked nipple)
- avoid: breastfeeding (HIV infection use in patients with bleeding nipple)
- avoid: breastfeeding (HIV infection use in patients with mastitis)
- caution: acute HIV infection, suspected (HIV pre-exposure prophylaxis use)
Drug Interactions .
Overview
lenacapavir
HIV capsid inhibitor
- CYP3A4 substrate
- UGT1A1 substrate
- P-gp substrate
- CYP3A4 inhibitor, moderate
- BCRP inhibitor
- P-gp inhibitor, weak
- affected by altered fat absorption
- lenacapavir is indicated for treatment of HIV infection (Sunlenca; Bixlenvo in combination w/ bictegravir) and HIV pre-exposure prophylaxis (Yeztugo); drug interaction guidance with strong and moderate CYP3A4 inducers varies by indication; see individual drug interactions for specific details
Contraindicated
Avoid/Use Alternative
Monitor/Modify Tx
Caution Advised
Adverse Reactions .
Serious Reactions
- immune reconstitution syndrome (HIV infection use)
- autoimmune disorders (HIV infection use)
- injection site necrosis
Common Reactions
- injection site reaction
- headache
- nausea
- dizziness
- vomiting
- diarrhea
- Cr incr.
- glycosuria
- hyperglycemia
- proteinuria
- ALT or AST incr.
- bilirubin incr.
Safety/Monitoring .
Monitoring Parameters
no routine tests recommended
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; risk of fetal harm not expected based on limited human data; no known risk of fetal harm based on animal data at 21x and 170x systemic exposure
Pregnancy Registry
enroll patients in Antiretroviral Pregnancy Registry at 1-800-258-4263; additional info at www.apregistry.com
Lactation
Clinical Summary
weigh risk/benefit while breastfeeding; no known risk of infant harm based on limited human data; no human data available to assess effects on milk production
Pharmacology .
Metabolism: for lenacapavir: liver; CYP450: 3A substrate (minor); UGT: 1A1 substrate (minor)
Excretion: for lenacapavir: feces 76% (33% unchanged), urine <1% ; Half-life: 10-12 days (PO); 8-12 wk (SC)
Subclass: HIV: Capsid Inhibitors
Mechanism of Action
for lenacapavir: binds to HIV capsid protein subunits, inhibiting HIV replication by interfering with multiple essential steps of viral lifecycle
Formulary .
No Formulary Selected
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