Peringatan Keamanan

Data regarding overdoses of remdesivir are not readily available.L13239 Overdoses of other nucleoside analogs like acyclovir can be managed with symptomatic and supportive treatment.A191472

Remdesivir

DB14761

small molecule approved investigational

Deskripsi

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the causative agent of coronavirus disease 2019 (COVID-19), which is a respiratory disease that is capable of progressing to viral pneumonia and acute respiratory distress syndrome (ARDS); COVID-19 can be fatal. Like other RNA viruses, SARS-CoV-2 depends on an RNA-dependent RNA polymerase (RdRp) enzyme complex for genomic replication, which can be inhibited by a class of drugs known as nucleoside analogues.A222398

Remdesivir (GS-5734) is an adenosine triphosphate analogue first described in the literature in 2016 as a potential treatment for Ebola.A191379, A222393 Broad antiviral activity of remdesivir is suggested by its mechanism of action,A222398 and to date, it has demonstrated in vitro activity against the Arenaviridae, Flaviviridae, Filoviridae, Paramyxoviridae, Pneumoviridae, and Coronaviridae viral families.A222393 Remdesivir activity against the Coronaviridae family was first demonstrated in 2017,A191382 leading to considerable interest in remdesivir as a possible treatment for COVID-19.A191427, A198810 Remdesivir was confirmed as a non-obligate chain terminator of RdRp from SARS-CoV-2 and the related SARS-CoV and MERS-CoV,A222398 and has been investigated in multiple COVID-19 clinical trials.L12174, L12177

After initially being granted an FDA Emergency Use Authorization (EUA) on May 1st, 2020,L13236 remdesivir was fully approved by the FDA for the treatment of COVID-19 on October 22, 2020.L18438 Remdesivir is currently marketed under the trademark name VEKLURY by Gilead Sciences Inc.L18438 Remdesivir was also approved by the European Commission on July 3, 2020.L39640 Remdesivir in combination with baricitinib for the treatment of COVID-19, was granted an FDA Emergency Use Authorization on November 19, 2020.L22619

Struktur Molekul 2D

Berat 602.585
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Remdesivir has an elimination half-life of 1 hour following a single 30-minute intravenous infusion. Under the same conditions, the elimination half-lives of the remdesivir metabolites [GS-441524] and GS-704277 are 27 hours and 1.3 hours, respectively.[L18438] A 10mg/kg intravenous dose in non-human primates has a plasma half-life of 0.39h.[A191379] The nucleoside triphosphate metabolite has a half-life of 14h in non-human primates.[A191379] The nucleoside triphosphate metabolite has a half-life of approximately 20 hours in humans.[A191382]
Volume Distribusi Data regarding the volume of distribution of remdesivir is not readily available.
Klirens (Clearance) Data regarding the clearance of remdesivir is not readily available.

Absorpsi

Remdesivir is absorbed quickly; maximal plasma concentrations following a single 30-minute intravenous infusion are reached within 0.67-0.68 hours (Tmax). Repeated dosing yields a Cmax (coefficient of variation as a percent) of 2229 (19.2) ng/mL and an AUCtau of 1585 (16.6) ng\*h/mL.L18438 Remdesivir metabolite GS-441524 has measured values: Tmax 1.51-2.00 hours, Cmax 145 (19.3) ng/mL, AUCtau 2229 (18.4) ng\*h/mL, and Ctrough 69.2 (18.2) ng/mL. Another metabolite, GS-704277, has measured values: Tmax 0.75 hours, Cmax 246 (33.9) ng/mL, AUCtau 462 (31.4) ng\*h/mL, and an undetermined Ctrough.L18438 A 10mg/kg intravenous dose given to cynomolgus monkeys distributes to the testes, epididymis, eyes, and brain within 4h.A191379

Metabolisme

Remdesivir is a phosphoramidate prodrug that must be metabolized within host cells to its triphosphate metabolite to be therapeutically active.A191379, A191382, A222468 Upon cell entry, remdesivir is presumed to undergo first esterase-mediated hydrolysis to a carboxylate form followed by cyclization to eject the phenoxide moiety and finally hydrolysis of the cyclic anhydride to yield the detectable alanine metabolite (GS-704277).A222468 The alanine metabolite is subsequently hydrolyzed to yield the monophosphate form of remdesivir, which is either hydrolyzed again to yield the bare nucleoside metabolite GS-441524 or phosphorylated by cellular kinases to yield the active triphosphate form.A191379, A222468

Rute Eliminasi

Remdesivir is 74% eliminated in the urine and 18% eliminated in the feces.L13239 49% of the recovered dose is in the form of the metabolite GS-441524, and 10% is recovered as the unmetabolized parent compound.L13239 A small amount (0.5%) of the GS-441524 metabolite is found in feces.L18438

Interaksi Obat

329 Data
Lomitapide The metabolism of Lomitapide can be decreased when combined with Remdesivir.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Remdesivir.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Remdesivir.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Remdesivir.
Colchicine The metabolism of Colchicine can be decreased when combined with Remdesivir.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Remdesivir.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Remdesivir.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Remdesivir.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Remdesivir.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Remdesivir.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Remdesivir.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Remdesivir.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Remdesivir.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Remdesivir.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Remdesivir.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Remdesivir.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Remdesivir.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Remdesivir.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Remdesivir.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Remdesivir.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Remdesivir.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Remdesivir.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Remdesivir.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Remdesivir.
Vemurafenib The metabolism of Vemurafenib can be decreased when combined with Remdesivir.
Apalutamide The serum concentration of Remdesivir can be decreased when it is combined with Apalutamide.
Cholic Acid The excretion of Remdesivir can be increased when combined with Cholic Acid.
Taurocholic acid The excretion of Remdesivir can be increased when combined with Taurocholic acid.
Pitolisant The serum concentration of Remdesivir can be decreased when it is combined with Pitolisant.
Isavuconazonium The metabolism of Remdesivir can be decreased when combined with Isavuconazonium.
Isavuconazole The metabolism of Remdesivir can be decreased when combined with Isavuconazole.
Fluconazole The metabolism of Remdesivir can be decreased when combined with Fluconazole.
Erythromycin The serum concentration of Remdesivir can be increased when it is combined with Erythromycin.
Verapamil The metabolism of Remdesivir can be decreased when combined with Verapamil.
Simeprevir The metabolism of Remdesivir can be decreased when combined with Simeprevir.
Linagliptin The metabolism of Remdesivir can be decreased when combined with Linagliptin.
Vorapaxar The metabolism of Vorapaxar can be decreased when combined with Remdesivir.
Suvorexant The metabolism of Suvorexant can be decreased when combined with Remdesivir.
Netupitant The metabolism of Remdesivir can be decreased when combined with Netupitant.
Voxilaprevir The excretion of Voxilaprevir can be decreased when combined with Remdesivir.
Glecaprevir The excretion of Glecaprevir can be decreased when combined with Remdesivir.
Levoketoconazole The metabolism of Remdesivir can be decreased when combined with Levoketoconazole.
Aripiprazole The metabolism of Aripiprazole can be decreased when combined with Remdesivir.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be decreased when combined with Remdesivir.
Valsartan The excretion of Valsartan can be decreased when combined with Remdesivir.
Conjugated estrogens The excretion of Conjugated estrogens can be decreased when combined with Remdesivir.
Caspofungin The excretion of Caspofungin can be decreased when combined with Remdesivir.
Ouabain The excretion of Ouabain can be decreased when combined with Remdesivir.
Fluvastatin The excretion of Fluvastatin can be decreased when combined with Remdesivir.
Rosuvastatin The metabolism of Rosuvastatin can be decreased when combined with Remdesivir.
Cholecystokinin The excretion of Cholecystokinin can be decreased when combined with Remdesivir.
Bempedoic acid The excretion of Bempedoic acid can be decreased when combined with Remdesivir.
Liothyronine The excretion of Liothyronine can be decreased when combined with Remdesivir.
Raloxifene The excretion of Raloxifene can be decreased when combined with Remdesivir.
Mycophenolate mofetil The excretion of Mycophenolate mofetil can be decreased when combined with Remdesivir.
Liotrix The excretion of Liotrix can be decreased when combined with Remdesivir.
Gadoxetic acid The excretion of Gadoxetic acid can be decreased when combined with Remdesivir.
Technetium Tc-99m mebrofenin The excretion of Technetium Tc-99m mebrofenin can be decreased when combined with Remdesivir.
Tenofovir alafenamide The metabolism of Tenofovir alafenamide can be decreased when combined with Remdesivir.
Letermovir The excretion of Letermovir can be decreased when combined with Remdesivir.
Levosalbutamol The excretion of Levosalbutamol can be decreased when combined with Remdesivir.
Elexacaftor The serum concentration of Remdesivir can be increased when it is combined with Elexacaftor.
Metreleptin The metabolism of Remdesivir can be increased when combined with Metreleptin.
Azithromycin The metabolism of Azithromycin can be decreased when combined with Remdesivir.
Methysergide The metabolism of Methysergide can be decreased when combined with Remdesivir.
Meperidine The metabolism of Meperidine can be decreased when combined with Remdesivir.
Chlorpromazine The metabolism of Chlorpromazine can be decreased when combined with Remdesivir.
Albendazole The metabolism of Albendazole can be decreased when combined with Remdesivir.
Doxazosin The metabolism of Doxazosin can be decreased when combined with Remdesivir.
Cisapride The metabolism of Cisapride can be decreased when combined with Remdesivir.
Norethisterone The metabolism of Norethisterone can be decreased when combined with Remdesivir.
Fenofibrate The metabolism of Fenofibrate can be decreased when combined with Remdesivir.
Drospirenone The metabolism of Drospirenone can be decreased when combined with Remdesivir.
Allylestrenol The metabolism of Allylestrenol can be decreased when combined with Remdesivir.
Zuclopenthixol The metabolism of Zuclopenthixol can be decreased when combined with Remdesivir.
Roflumilast The serum concentration of Roflumilast can be increased when it is combined with Remdesivir.
Lacosamide The metabolism of Lacosamide can be decreased when combined with Remdesivir.
Fosaprepitant The metabolism of Fosaprepitant can be decreased when combined with Remdesivir.
Tasimelteon The metabolism of Tasimelteon can be decreased when combined with Remdesivir.
Dihydroergocornine The metabolism of Dihydroergocornine can be decreased when combined with Remdesivir.
Ebastine The metabolism of Ebastine can be decreased when combined with Remdesivir.
9-aminocamptothecin The metabolism of 9-aminocamptothecin can be decreased when combined with Remdesivir.
Methylprednisone The metabolism of Methylprednisone can be decreased when combined with Remdesivir.
Dihydroergocristine The metabolism of Dihydroergocristine can be decreased when combined with Remdesivir.
Dihydroergocryptine The metabolism of Dihydroergocryptine can be decreased when combined with Remdesivir.
Medical Cannabis The metabolism of Medical Cannabis can be decreased when combined with Remdesivir.
Pretomanid The metabolism of Pretomanid can be decreased when combined with Remdesivir.
Pimavanserin The metabolism of Pimavanserin can be decreased when combined with Remdesivir.
Estetrol The metabolism of Estetrol can be decreased when combined with Remdesivir.
Infigratinib The metabolism of Infigratinib can be decreased when combined with Remdesivir.
Cyclosporine The metabolism of Cyclosporine can be decreased when combined with Remdesivir.
Sorafenib The metabolism of Sorafenib can be decreased when combined with Remdesivir.
Tamoxifen The metabolism of Tamoxifen can be decreased when combined with Remdesivir.
Quinidine The metabolism of Quinidine can be decreased when combined with Remdesivir.
Dronedarone The metabolism of Dronedarone can be decreased when combined with Remdesivir.
Vandetanib The metabolism of Vandetanib can be decreased when combined with Remdesivir.
Temsirolimus The metabolism of Temsirolimus can be decreased when combined with Remdesivir.
Crizotinib The metabolism of Crizotinib can be decreased when combined with Remdesivir.
Regorafenib The metabolism of Regorafenib can be decreased when combined with Remdesivir.
Ponatinib The metabolism of Ponatinib can be decreased when combined with Remdesivir.

Target Protein

Replicase polyprotein 1ab rep
Replicase polyprotein 1ab rep
Replicase polyprotein 1ab rep
RNA-directed RNA polymerase L L

Referensi & Sumber

Synthesis reference: Byoung Kwon Chun, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Hon Chung Hui, Robert Jordan, Richard L. Mackman, Jay P. Parrish, Adrian S. Ray, and Dustin Siegel, "Methods for treating Filoviridae virus infections." U.S. Patent US9724360B2, issued August 8, 2017.
Artikel (PubMed)
  • PMID: 26934220
    Warren TK, Jordan R, Lo MK, Ray AS, Mackman RL, Soloveva V, Siegel D, Perron M, Bannister R, Hui HC, Larson N, Strickley R, Wells J, Stuthman KS, Van Tongeren SA, Garza NL, Donnelly G, Shurtleff AC, Retterer CJ, Gharaibeh D, Zamani R, Kenny T, Eaton BP, Grimes E, Welch LS, Gomba L, Wilhelmsen CL, Nichols DK, Nuss JE, Nagle ER, Kugelman JR, Palacios G, Doerffler E, Neville S, Carra E, Clarke MO, Zhang L, Lew W, Ross B, Wang Q, Chun K, Wolfe L, Babusis D, Park Y, Stray KM, Trancheva I, Feng JY, Barauskas O, Xu Y, Wong P, Braun MR, Flint M, McMullan LK, Chen SS, Fearns R, Swaminathan S, Mayers DL, Spiropoulou CF, Lee WA, Nichol ST, Cihlar T, Bavari S: Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys. Nature. 2016 Mar 17;531(7594):381-5. doi: 10.1038/nature17180. Epub 2016 Mar 2.
  • PMID: 28659436
    Sheahan TP, Sims AC, Graham RL, Menachery VD, Gralinski LE, Case JB, Leist SR, Pyrc K, Feng JY, Trantcheva I, Bannister R, Park Y, Babusis D, Clarke MO, Mackman RL, Spahn JE, Palmiotti CA, Siegel D, Ray AS, Cihlar T, Jordan R, Denison MR, Baric RS: Broad-spectrum antiviral GS-5734 inhibits both epidemic and zoonotic coronaviruses. Sci Transl Med. 2017 Jun 28;9(396). pii: 9/396/eaal3653. doi: 10.1126/scitranslmed.aal3653.
  • PMID: 29511076
    Agostini ML, Andres EL, Sims AC, Graham RL, Sheahan TP, Lu X, Smith EC, Case JB, Feng JY, Jordan R, Ray AS, Cihlar T, Siegel D, Mackman RL, Clarke MO, Baric RS, Denison MR: Coronavirus Susceptibility to the Antiviral Remdesivir (GS-5734) Is Mediated by the Viral Polymerase and the Proofreading Exoribonuclease. mBio. 2018 Mar 6;9(2). pii: mBio.00221-18. doi: 10.1128/mBio.00221-18.
  • PMID: 32054787
    de Wit E, Feldmann F, Cronin J, Jordan R, Okumura A, Thomas T, Scott D, Cihlar T, Feldmann H: Prophylactic and therapeutic remdesivir (GS-5734) treatment in the rhesus macaque model of MERS-CoV infection. Proc Natl Acad Sci U S A. 2020 Feb 13. pii: 1922083117. doi: 10.1073/pnas.1922083117.
  • PMID: 12799156
    Vander T, Medvedovsky M, Herishanu Y: Encephalopathy induced by oral acyclovir in a patient with normal renal function. J Infect. 2003 May;46(4):286. doi: 10.1053/jinf.2002.1119.
  • PMID: 32147516
    Ko WC, Rolain JM, Lee NY, Chen PL, Huang CT, Lee PI, Hsueh PR: Arguments in favor of remdesivir for treating SARS-CoV-2 infections. Int J Antimicrob Agents. 2020 Mar 5:105933. doi: 10.1016/j.ijantimicag.2020.105933.
  • PMID: 32275812
    Grein J, Ohmagari N, Shin D, Diaz G, Asperges E, Castagna A, Feldt T, Green G, Green ML, Lescure FX, Nicastri E, Oda R, Yo K, Quiros-Roldan E, Studemeister A, Redinski J, Ahmed S, Bernett J, Chelliah D, Chen D, Chihara S, Cohen SH, Cunningham J, D'Arminio Monforte A, Ismail S, Kato H, Lapadula G, L'Her E, Maeno T, Majumder S, Massari M, Mora-Rillo M, Mutoh Y, Nguyen D, Verweij E, Zoufaly A, Osinusi AO, DeZure A, Zhao Y, Zhong L, Chokkalingam A, Elboudwarej E, Telep L, Timbs L, Henne I, Sellers S, Cao H, Tan SK, Winterbourne L, Desai P, Mera R, Gaggar A, Myers RP, Brainard DM, Childs R, Flanigan T: Compassionate Use of Remdesivir for Patients with Severe Covid-19. N Engl J Med. 2020 Apr 10. doi: 10.1056/NEJMoa2007016.
  • PMID: 32350436
    Ledford H: Hopes rise on coronavirus drug remdesivir. Nature. 2020 Apr 29. pii: 10.1038/d41586-020-01295-8. doi: 10.1038/d41586-020-01295-8.
Menampilkan 8 dari 11 artikel.

Contoh Produk & Brand

Produk: 6 • International brands: 0
Produk
  • Veklury
    Injection • 5 mg/1mL • Intravenous • US • Approved
  • Veklury
    Injection, powder, lyophilized, for solution • 100 mg/1 • Intravenous • US • Approved
  • Veklury
    Solution • 100 mg / 20 mL • Intravenous • Canada • Approved
  • Veklury
    Powder, for solution • 100 mg / vial • Intravenous • Canada • Approved
  • Veklury
    Injection, solution, concentrate • 100 mg • Intravenous • EU • Approved
  • Veklury
    Injection, powder, for solution • 100 mg • Intravenous • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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