Peringatan Keamanan

There is limited information available regarding the acute toxicity and overdose of lenacapavir. If overdose occurs the patient must be monitored for signs or symptoms of adverse reactions. Treatment of overdose with lenacapavir consists of general supportive measures including monitoring of vital signs as well as observation of the clinical status of the patient. As lenacapavir is highly protein bound, it is unlikely to be significantly removed by dialysis.L42990

Lenacapavir

DB15673

small molecule approved investigational

Deskripsi

HIV/AIDS remains an area of concern despite the introduction of numerous successful therapies, mainly due to the emergence of multidrug resistance and patient difficulty in adhering to treatment regimens.A244170, A244175 Lenacapavir is a first-in-class capsid inhibitor that demonstrates picomolar HIV-1 inhibition as a monotherapy in vitro, little to no cross-resistance with existing antiretroviral agents, and extended pharmacokinetics with subcutaneous dosing.A244170, A244175, A244180, A244190

Lenacapavir was first globally approved on August 22, 2022 by the European Commission to treat adults with multi-drug resistant HIV infection.L42995 On December 22, 2022, it was also approved by the FDA.L44473

Struktur Molekul 2D

Berat 968.28
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The median half-life ranged from 10 to 12 days following following oral administration, and 8 to 12 weeks following subcutaneous administration.[L42990]
Volume Distribusi The steady state volume of distribution was 976 L in heavily treatment-experienced patients with an HIV-1 infection.[L42990]
Klirens (Clearance) Lenacapavir clearance was 3.62 L/h in heavily treatment experienced patients with HIV-1 infection.[L42990]

Absorpsi

Following subcutaneous administration, lenacapavir is slowly released but completely absorbed, with peak plasma concentrations occurring at 84 days post-dose. Absolute bioavailability following oral administration is low, approximately 6 to 10%. Tmax after oral administration is about four hours. The mean steady-state Cmax (%CV) is 97.2 (70.3) ng/ mL following oral and subcutaneous administration.L42990 According to population pharmacokinetics analysis, lenacapavir exposures (AUCtau, Cmax and Ctrough) were 29% to 84% higher in heavily treatment-experienced patients with an HIV-1 infection compared to subjects without an HIV-1 infection. A low-fat meal had negligible effects on drug absorption.L42990

Metabolisme

Metabolism played a lesser role in lenacapavir elimination. It undergoes CYP3A4- and UGT1A1-mediated oxidation, N-dealkylation, hydrogenation, amide hydrolysis, glucuronidation, hexose conjugation, pentose conjugation, and glutathione conjugation. The metabolites of lenacapavir have not been fully characterized. No single circulating metabolite accounted for >10% of plasma drug-related exposure.L42990

Rute Eliminasi

Following a single intravenous dose of radiolabelled-lenacapavir in healthy subjects, 76% of the total radioactivity was recovered from feces and less than 1% from urine. Unchanged lenacapavir was the predominant moiety in plasma (69%) and feces (33%).L42990

Interaksi Makanan

1 Data
  • 1. Take with or without food. Oral lenacapavir should be taken orally with or without food, as food has negligible effects on drug absorption.

Interaksi Obat

390 Data
Rubella virus vaccine The therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Lenacapavir.
Varicella zoster vaccine (live/attenuated) The therapeutic efficacy of Varicella zoster vaccine (live/attenuated) can be decreased when used in combination with Lenacapavir.
Bacillus calmette-guerin substrain tice live antigen The therapeutic efficacy of Bacillus calmette-guerin substrain tice live antigen can be decreased when used in combination with Lenacapavir.
Bacillus calmette-guerin substrain connaught live antigen The therapeutic efficacy of Bacillus calmette-guerin substrain connaught live antigen can be decreased when used in combination with Lenacapavir.
Yellow fever vaccine The therapeutic efficacy of Yellow fever vaccine can be decreased when used in combination with Lenacapavir.
Anthrax vaccine The therapeutic efficacy of Anthrax vaccine can be decreased when used in combination with Lenacapavir.
Typhoid Vaccine Live The therapeutic efficacy of Typhoid Vaccine Live can be decreased when used in combination with Lenacapavir.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Lenacapavir.
Human adenovirus e serotype 4 strain cl-68578 antigen The therapeutic efficacy of Human adenovirus e serotype 4 strain cl-68578 antigen can be decreased when used in combination with Lenacapavir.
Vibrio cholerae CVD 103-HgR strain live antigen The therapeutic efficacy of Vibrio cholerae CVD 103-HgR strain live antigen can be decreased when used in combination with Lenacapavir.
Adenovirus type 7 vaccine live The therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Lenacapavir.
Bacillus calmette-guerin substrain russian BCG-I live antigen The therapeutic efficacy of Bacillus calmette-guerin substrain russian BCG-I live antigen can be decreased when used in combination with Lenacapavir.
Phenytoin The metabolism of Lenacapavir can be increased when combined with Phenytoin.
Pentobarbital The metabolism of Lenacapavir can be increased when combined with Pentobarbital.
Carbamazepine The metabolism of Lenacapavir can be increased when combined with Carbamazepine.
Mitotane The metabolism of Lenacapavir can be increased when combined with Mitotane.
Primidone The metabolism of Lenacapavir can be increased when combined with Primidone.
Rimexolone The metabolism of Lenacapavir can be increased when combined with Rimexolone.
Rifampin The metabolism of Lenacapavir can be increased when combined with Rifampicin.
Phenobarbital The metabolism of Lenacapavir can be increased when combined with Phenobarbital.
Rifapentine The metabolism of Lenacapavir can be increased when combined with Rifapentine.
Dexamethasone The metabolism of Lenacapavir can be increased when combined with Dexamethasone.
Fosphenytoin The metabolism of Lenacapavir can be increased when combined with Fosphenytoin.
St. John's Wort The metabolism of Lenacapavir can be increased when combined with St. John's Wort.
Midostaurin The metabolism of Lenacapavir can be increased when combined with Midostaurin.
Enzalutamide The metabolism of Lenacapavir can be increased when combined with Enzalutamide.
Lumacaftor The metabolism of Lenacapavir can be increased when combined with Lumacaftor.
Apalutamide The metabolism of Lenacapavir can be increased when combined with Apalutamide.
Nelfinavir The metabolism of Lenacapavir can be increased when combined with Nelfinavir.
Desogestrel The metabolism of Lenacapavir can be increased when combined with Desogestrel.
Zidovudine The metabolism of Lenacapavir can be increased when combined with Zidovudine.
Ritonavir The metabolism of Lenacapavir can be increased when combined with Ritonavir.
Lamotrigine The metabolism of Lenacapavir can be increased when combined with Lamotrigine.
Efavirenz The metabolism of Lenacapavir can be increased when combined with Efavirenz.
Tipranavir The metabolism of Lenacapavir can be increased when combined with Tipranavir.
Ethinylestradiol The metabolism of Lenacapavir can be increased when combined with Ethinylestradiol.
Testosterone propionate The metabolism of Lenacapavir can be increased when combined with Testosterone propionate.
Mitapivat The metabolism of Lenacapavir can be increased when combined with Mitapivat.
Levothyroxine The serum concentration of Lenacapavir can be decreased when it is combined with Levothyroxine.
Trazodone The serum concentration of Lenacapavir can be decreased when it is combined with Trazodone.
Mifepristone The serum concentration of Lenacapavir can be decreased when it is combined with Mifepristone.
Lorlatinib The serum concentration of Lenacapavir can be decreased when it is combined with Lorlatinib.
Prednisolone phosphate The serum concentration of Lenacapavir can be decreased when it is combined with Prednisolone phosphate.
Dexamethasone acetate The serum concentration of Lenacapavir can be decreased when it is combined with Dexamethasone acetate.
Cyclosporine The metabolism of Cyclosporine can be decreased when combined with Lenacapavir.
Bortezomib The metabolism of Bortezomib can be decreased when combined with Lenacapavir.
Dofetilide The metabolism of Dofetilide can be decreased when combined with Lenacapavir.
Cabergoline The metabolism of Cabergoline can be decreased when combined with Lenacapavir.
Theophylline The metabolism of Theophylline can be decreased when combined with Lenacapavir.
Vindesine The metabolism of Vindesine can be decreased when combined with Lenacapavir.
Dihydroergotamine The metabolism of Dihydroergotamine can be decreased when combined with Lenacapavir.
Vinorelbine The metabolism of Vinorelbine can be decreased when combined with Lenacapavir.
Sorafenib The metabolism of Sorafenib can be decreased when combined with Lenacapavir.
Teniposide The metabolism of Teniposide can be decreased when combined with Lenacapavir.
Erlotinib The metabolism of Erlotinib can be decreased when combined with Lenacapavir.
Cyclophosphamide The metabolism of Cyclophosphamide can be decreased when combined with Lenacapavir.
Nortriptyline The metabolism of Nortriptyline can be decreased when combined with Lenacapavir.
Vincristine The metabolism of Vincristine can be decreased when combined with Lenacapavir.
Methotrexate The metabolism of Methotrexate can be decreased when combined with Lenacapavir.
Vinblastine The metabolism of Vinblastine can be decreased when combined with Lenacapavir.
Clonidine The metabolism of Clonidine can be decreased when combined with Lenacapavir.
Astemizole The metabolism of Astemizole can be decreased when combined with Lenacapavir.
Tamoxifen The metabolism of Tamoxifen can be decreased when combined with Lenacapavir.
Warfarin The metabolism of Warfarin can be decreased when combined with Lenacapavir.
Ergotamine The metabolism of Ergotamine can be decreased when combined with Lenacapavir.
Irinotecan The metabolism of Irinotecan can be decreased when combined with Lenacapavir.
Etoposide The metabolism of Etoposide can be decreased when combined with Lenacapavir.
Tacrolimus The metabolism of Tacrolimus can be decreased when combined with Lenacapavir.
Conivaptan The metabolism of Conivaptan can be decreased when combined with Lenacapavir.
Sirolimus The metabolism of Sirolimus can be decreased when combined with Lenacapavir.
Quinidine The metabolism of Quinidine can be decreased when combined with Lenacapavir.
Phenprocoumon The metabolism of Phenprocoumon can be decreased when combined with Lenacapavir.
Doxorubicin The metabolism of Doxorubicin can be decreased when combined with Lenacapavir.
Busulfan The metabolism of Busulfan can be decreased when combined with Lenacapavir.
Pimozide The metabolism of Pimozide can be decreased when combined with Lenacapavir.
Amiodarone The metabolism of Amiodarone can be decreased when combined with Lenacapavir.
Bicalutamide The metabolism of Bicalutamide can be decreased when combined with Lenacapavir.
Ifosfamide The metabolism of Ifosfamide can be decreased when combined with Lenacapavir.
Aminophylline The metabolism of Aminophylline can be decreased when combined with Lenacapavir.
Levacetylmethadol The metabolism of Levacetylmethadol can be decreased when combined with Lenacapavir.
Paclitaxel The metabolism of Paclitaxel can be decreased when combined with Lenacapavir.
Clomipramine The metabolism of Clomipramine can be decreased when combined with Lenacapavir.
Docetaxel The metabolism of Docetaxel can be decreased when combined with Lenacapavir.
Dasatinib The metabolism of Dasatinib can be decreased when combined with Lenacapavir.
Sunitinib The metabolism of Sunitinib can be decreased when combined with Lenacapavir.
Digitoxin The metabolism of Digitoxin can be decreased when combined with Lenacapavir.
Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Lenacapavir.
Everolimus The metabolism of Everolimus can be decreased when combined with Lenacapavir.
Thiotepa The metabolism of Thiotepa can be decreased when combined with Lenacapavir.
Ixabepilone The metabolism of Ixabepilone can be decreased when combined with Lenacapavir.
Dronedarone The metabolism of Dronedarone can be decreased when combined with Lenacapavir.
Nilotinib The metabolism of Nilotinib can be decreased when combined with Lenacapavir.
Trabectedin The metabolism of Trabectedin can be decreased when combined with Lenacapavir.
Cobimetinib The metabolism of Cobimetinib can be decreased when combined with Lenacapavir.
Vandetanib The metabolism of Vandetanib can be decreased when combined with Lenacapavir.
Trastuzumab emtansine The metabolism of Trastuzumab emtansine can be decreased when combined with Lenacapavir.
Romidepsin The metabolism of Romidepsin can be decreased when combined with Lenacapavir.
Tolvaptan The metabolism of Tolvaptan can be decreased when combined with Lenacapavir.
Temsirolimus The metabolism of Temsirolimus can be decreased when combined with Lenacapavir.
Pazopanib The metabolism of Pazopanib can be decreased when combined with Lenacapavir.

Target Protein

Gag-Pol polyprotein gag-pol

Referensi & Sumber

Artikel (PubMed)
  • PMID: 33807824
    Zhuang S, Torbett BE: Interactions of HIV-1 Capsid with Host Factors and Their Implications for Developing Novel Therapeutics. Viruses. 2021 Mar 5;13(3). pii: v13030417. doi: 10.3390/v13030417.
  • PMID: 32612233
    Link JO, Rhee MS, Tse WC, Zheng J, Somoza JR, Rowe W, Begley R, Chiu A, Mulato A, Hansen D, Singer E, Tsai LK, Bam RA, Chou CH, Canales E, Brizgys G, Zhang JR, Li J, Graupe M, Morganelli P, Liu Q, Wu Q, Halcomb RL, Saito RD, Schroeder SD, Lazerwith SE, Bondy S, Jin D, Hung M, Novikov N, Liu X, Villasenor AG, Cannizzaro CE, Hu EY, Anderson RL, Appleby TC, Lu B, Mwangi J, Liclican A, Niedziela-Majka A, Papalia GA, Wong MH, Leavitt SA, Xu Y, Koditek D, Stepan GJ, Yu H, Pagratis N, Clancy S, Ahmadyar S, Cai TZ, Sellers S, Wolckenhauer SA, Ling J, Callebaut C, Margot N, Ram RR, Liu YP, Hyland R, Sinclair GI, Ruane PJ, Crofoot GE, McDonald CK, Brainard DM, Lad L, Swaminathan S, Sundquist WI, Sakowicz R, Chester AE, Lee WE, Daar ES, Yant SR, Cihlar T: Clinical targeting of HIV capsid protein with a long-acting small molecule. Nature. 2020 Aug;584(7822):614-618. doi: 10.1038/s41586-020-2443-1. Epub 2020 Jul 1.
  • PMID: 33060363
    Bester SM, Wei G, Zhao H, Adu-Ampratwum D, Iqbal N, Courouble VV, Francis AC, Annamalai AS, Singh PK, Shkriabai N, Van Blerkom P, Morrison J, Poeschla EM, Engelman AN, Melikyan GB, Griffin PR, Fuchs JR, Asturias FJ, Kvaratskhelia M: Structural and mechanistic bases for a potent HIV-1 capsid inhibitor. Science. 2020 Oct 16;370(6514):360-364. doi: 10.1126/science.abb4808.
  • PMID: 31312185
    Singh K, Gallazzi F, Hill KJ, Burke DH, Lange MJ, Quinn TP, Neogi U, Sonnerborg A: GS-CA Compounds: First-In-Class HIV-1 Capsid Inhibitors Covering Multiple Grounds. Front Microbiol. 2019 Jun 20;10:1227. doi: 10.3389/fmicb.2019.01227. eCollection 2019.
  • PMID: 33288639
    Margot N, Ram R, Rhee M, Callebaut C: Absence of Lenacapavir (GS-6207) Phenotypic Resistance in HIV Gag Cleavage Site Mutants and in Isolates with Resistance to Existing Drug Classes. Antimicrob Agents Chemother. 2021 Feb 17;65(3). pii: AAC.02057-20. doi: 10.1128/AAC.02057-20. Print 2021 Feb 17.

Contoh Produk & Brand

Produk: 6 • International brands: 0
Produk
  • Sunlenca
    Tablet, film coated • 300 mg/1 • Oral • US • Approved
  • Sunlenca
    Injection; Kit • 463.5 mg/1.5mL • Subcutaneous • US • Approved
  • Sunlenca
    Tablet, film coated • 300 mg • Oral • EU • Approved
  • Sunlenca
    Injection, solution • 464 mg • Subcutaneous • EU • Approved
  • Sunlenca
    Tablet • 300 mg • Oral • Canada • Approved
  • Sunlenca
    Solution • 309 mg / mL • Subcutaneous • Canada • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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