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Yeztugo
lenacapavir
Black Box Warnings .
Drug Resistance Risk in Undiagnosed HIV-1 Infection
test pts for HIV-1 infection prior to starting lenacapavir and w/ each subsequent injection; drug-resistant variants identified in pts w/ undiagnosed HIV-1 infection; do not start lenacapavir unless negative HIV-1 infection status confirmed; pts infected w/ 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 w/ HIV-1 RNA before tx start and w/ 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 w/ HIV-1 RNA before tx start and w/ 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 pts w/ non-virological suppression throughout 3rd trimester)
- avoid: breastfeeding (HIV infection use in pts w/ non-virological suppression postpartum)
- avoid: breastfeeding (HIV infection use in pts w/ cracked nipple)
- avoid: breastfeeding (HIV infection use in pts w/ bleeding nipple)
- avoid: breastfeeding (HIV infection use in pts w/ 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
Contraindicated
- apalutamide
- butalbital
- carbamazepine
- cisapride
- colchicine
- eliglustat
- encorafenib
- enzalutamide
- flibanserin
- fosphenytoin
- ivosidenib
- lomitapide
- lumacaftor/ivacaftor
- mitotane
- pentobarbital
- phenytoin
- primidone
- rifampin
- St. John's wort
Avoid/Use Alternative
- adagrasib
- alfentanil
- alpelisib
- alprazolam
- amiodarone
- aprepitant
- atazanavir
- avapritinib
- azithromycin
- belumosudil
- bisoprolol
- bosentan
- bosutinib
- brigatinib
- buspirone
- cannabidiol
- capivasertib
- carvedilol
- cenobamate
- ceritinib
- chloramphenicol
- cladribine oral
- clarithromycin
- cobicistat
- cobimetinib
- codeine
- conivaptan
- cyclosporine
- dabigatran
- dabrafenib
- danicopan
- defactinib
- dihydrocodeine
- dihydroergotamine
- diosmin
- disopyramide
- domperidone
- doxorubicin
- dronedarone
- efavirenz
- elacestrant
- ensartinib
- entrectinib
- ergotamine
- erythromycin
- etrasimod
- etravirine
- fentanyl
- fexinidazole
- fosaprepitant
- futibatinib
- gemfibrozil
- glecaprevir
- hydrocodone
- idelalisib
- itraconazole
- ivabradine
- ivacaftor
- ixabepilone
- ketoconazole
- lapatinib
- ledipasvir
- lemborexant
- levoketoconazole
- lonafarnib
- lopinavir/ritonavir
- lorlatinib
- lovastatin
- lurbinectedin
- macitentan
- mavacamten
- mavorixafor
- meperidine
- methylergonovine
- midazolam
- mifepristone
- mitapivat
- mobocertinib
- modafinil
- nafcillin
- naloxegol
- nefazodone
- nelfinavir
- neratinib
- nevirapine
- nirogacestat
- nisoldipine
- olaparib
- oliceridine
- omaveloxolone
- orlistat
- oxcarbazepine
- oxycodone
- pacritinib
- palovarotene
- pazopanib
- pemigatinib
- pexidartinib
- phenobarbital
- pibrentasvir
- pimozide
- posaconazole
- pralsetinib
- probenecid
- propafenone
- quinidine (antiarrhythmic)
- ranolazine
- regorafenib
- relugolix
- repotrectinib
- ribociclib
- rifabutin
- rifapentine
- rivaroxaban
- selpercatinib
- selumetinib
- simvastatin
- siponimod
- sirolimus albumin-bound
- sonidegib
- sorafenib
- sotorasib
- sufentanil
- tadalafil
- tazemetostat
- tepotinib
- tipranavir
- tolvaptan
- topotecan
- tramadol
- tucatinib
- turmeric
- vardenafil
- venetoclax
- verapamil
- vimseltinib
- voriconazole
- voxilaprevir
Monitor/Modify Tx
- abemaciclib
- acalabrutinib
- afatinib
- alfuzosin
- apixaban
- aripiprazole oral
- artemether/lumefantrine
- atorvastatin
- avanafil
- avatrombopag
- axitinib
- brexpiprazole
- bromocriptine
- budesonide
- buprenorphine
- butorphanol
- cabozantinib
- cariprazine
- cilostazol
- clonazepam
- clozapine
- copanlisib
- crizotinib
- daridorexant
- dasatinib
- deflazacort
- digoxin
- docetaxel
- dofetilide
- edoxaban
- elexacaftor/tezacaftor/ivacaftor
- enfortumab vedotin
- eplerenone
- erdafitinib
- estazolam
- estradiol (contraceptive)
- ethinyl estradiol (contraceptive)
- everolimus
- fedratinib
- felodipine
- finerenone
- fluvastatin
- gepirone
- gilteritinib
- glasdegib
- guanfacine
- hydrocortisone
- ibrutinib
- iloperidone
- imatinib
- irinotecan
- lefamulin
- lidocaine
- lumateperone
- lurasidone
- mefloquine
- methadone
- methotrexate
- midostaurin
- mitoxantrone
- morphine
- nifedipine
- nilotinib
- nimodipine
- nortriptyline
- osilodrostat
- palbociclib
- panobinostat
- pimavanserin
- pirtobrutinib
- ponatinib
- pravastatin
- quetiapine
- quinidine (CYP2D6 inhibitor)
- quinine
- quizartinib
- red yeast rice
- repaglinide
- rimegepant
- riociguat
- rosuvastatin
- ruxolitinib
- ruxolitinib topical
- sebetralstat
- sertraline
- sildenafil
- sirolimus
- sparsentan
- sunitinib
- suvorexant
- suzetrigine
- tacrolimus
- talazoparib
- tamsulosin
- temsirolimus
- tenofovir disoproxil
- tezacaftor/ivacaftor
- tofacitinib
- toremifene
- trabectedin
- trazodone
- triazolam
- ubrogepant
- vanzacaftor/tezacaftor/deutivacaftor
- vemurafenib
- vinblastine
- vincristine
- vinorelbine
- voclosporin
- warfarin
- zanubrutinib
Caution Advised
- aliskiren
- armodafinil
- avacopan
- belzutifan
- bexarotene
- budesonide rectal
- clobazam
- cortisone
- cyclophosphamide
- danshen
- darifenacin
- darolutamide
- dexamethasone
- dicloxacillin
- duvelisib
- echinacea
- elafibranor
- elagolix
- eletriptan
- enasidenib
- erlotinib
- eslicarbazepine acetate
- felbamate
- fosamprenavir
- garlic
- ginkgo
- ginseng, Asian
- glycerol phenylbutyrate
- grazoprevir
- griseofulvin
- ifosfamide
- isavuconazonium
- istradefylline
- larotrectinib
- maraviroc
- meropenem
- methylprednisolone
- naldemedine
- odevixibat
- olutasidenib
- ospemifene
- perampanel
- pioglitazone
- prednisone
- ritonavir
- roflumilast
- roflumilast topical
- rufinamide
- sarilumab
- saxagliptin
- seladelpar
- silodosin
- sirolimus topical
- somatropin
- stiripentol
- sulfasalazine
- sunvozertinib
- tecovirimat
- telotristat ethyl
- ticagrelor
- tocilizumab
- topiramate
- tovorafenib
- tretinoin
- upadacitinib
- vaborbactam
- valproic acid
- vamorolone
- vilazodone
- vorasidenib
Adverse Reactions .
Serious Reactions
- immune reconstitution syndrome (HIV infection use)
- autoimmune disorders (HIV infection use)
Common Reactions
- injection site rxn
- headache
- nausea
- dizziness
- vomiting
- diarrhea
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 16x and 39x recommended human dose
Pregnancy Registry
enroll pts in Antiretroviral Pregnancy Registry at 1-800-258-4263; additional info at www.apregistry.com
Lactation
Clinical Summary
weigh risk/benefit while breastfeeding; no human data available to assess risk of infant harm or effects on milk production
Pharmacology .
Metabolism: liver; CYP450: 3A substrate (minor); UGT: 1A1 substrate (minor)
Excretion: feces 76% (33% unchanged), urine <1% ; Half-life: 10-12 days (PO); 8-12 wk (SC)
Subclass: HIV: Capsid Inhibitors
Mechanism of Action
binds to HIV capsid protein subunits, inhibiting HIV replication by interfering w/ multiple essential steps of viral lifecycle
Formulary .
No Formulary Selected
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