Peringatan Keamanan

Data regarding overdoses of sotorasib are not readily available. However, in clinical trials, signs of dose limiting toxicity were not found.A235168 Patients experiencing an overdose may experience and increased risk and severity of adverse effects such as diarrhea, nausea, vomiting, fatigue, and elevated aminotransferase.A235168

Sotorasib

DB15569

small molecule approved investigational

Deskripsi

Sotorasib, also known as AMG-510, is an acrylamide-derived KRAS inhibitor developed by Amgen.A187547,A187556 It is indicated in the treatment of adult patients with KRAS G12C mutant non-small cell lung cancer.L34288 This mutation makes up >50% of all KRAS mutations.A187550 Mutant KRAS discovered in 1982 but was not considered a druggable target until the mid-2010s.A235168 It is the first experimental KRAS inhibitor.A187547 The drug MRTX849 is also currently being developed and has the same target.A187547

Sotorasib was granted FDA approval on May 28, 2021,L34288 followed by the European Commission's approval on January 10, 2022.L39675

Struktur Molekul 2D

Berat 560.606
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Sotorasib has a terminal elimination half life of 5.5 ± 1.8 hours.[A235168,L34288]
Volume Distribusi The volume of distribution of sotorasib is 211 L.[L34288]
Klirens (Clearance) Sotorasib has an apparent clearance at steady state of 26.2 L/h.[L34288]

Absorpsi

A 960 mg once daily dose of sotorasib reaches a Cmax of 7.50 µg/mL, with a median Tmax of 2.0 hours, and an AUC0-24h of 65.3 h\*µg/mL.A235168

Metabolisme

Sotorasib is predominantly metabolized through conjugation or by CYP3As.L34288

Rute Eliminasi

Sotorasib is 74% eliminated in the feces and 6% eliminated in the urine.L34288 53% of the dose recovered in the feces and 1% of the dose recovered in the urine is in the form of the unchanged parent compound.L34288

Interaksi Makanan

2 Data
  • 1. Avoid antacids. If coadministration cannot be avoided, take sotorasib 4 hours before or 10 hours after antacids.
  • 2. Take with or without food. Taking sotorasib with a high fat, high calorie meal increases total exposure to sotorasib by 25%.

Interaksi Obat

939 Data
Pantoprazole The therapeutic efficacy of Sotorasib can be decreased when used in combination with Pantoprazole.
Omeprazole The therapeutic efficacy of Sotorasib can be decreased when used in combination with Omeprazole.
Lansoprazole The therapeutic efficacy of Sotorasib can be decreased when used in combination with Lansoprazole.
Esomeprazole The therapeutic efficacy of Sotorasib can be decreased when used in combination with Esomeprazole.
Rabeprazole The therapeutic efficacy of Sotorasib can be decreased when used in combination with Rabeprazole.
Dexlansoprazole The therapeutic efficacy of Sotorasib can be decreased when used in combination with Dexlansoprazole.
Ilaprazole The therapeutic efficacy of Sotorasib can be decreased when used in combination with Ilaprazole.
Dexrabeprazole The therapeutic efficacy of Sotorasib can be decreased when used in combination with Dexrabeprazole.
Olanzapine The therapeutic efficacy of Sotorasib can be decreased when used in combination with Olanzapine.
Cimetidine The therapeutic efficacy of Sotorasib can be decreased when used in combination with Cimetidine.
Nizatidine The therapeutic efficacy of Sotorasib can be decreased when used in combination with Nizatidine.
Epinastine The therapeutic efficacy of Sotorasib can be decreased when used in combination with Epinastine.
Ranitidine The therapeutic efficacy of Sotorasib can be decreased when used in combination with Ranitidine.
Famotidine The therapeutic efficacy of Sotorasib can be decreased when used in combination with Famotidine.
Methantheline The therapeutic efficacy of Sotorasib can be decreased when used in combination with Methantheline.
Promethazine The therapeutic efficacy of Sotorasib can be decreased when used in combination with Promethazine.
Doxepin The therapeutic efficacy of Sotorasib can be decreased when used in combination with Doxepin.
Asenapine The therapeutic efficacy of Sotorasib can be decreased when used in combination with Asenapine.
Metiamide The therapeutic efficacy of Sotorasib can be decreased when used in combination with Metiamide.
Roxatidine acetate The therapeutic efficacy of Sotorasib can be decreased when used in combination with Roxatidine acetate.
Lafutidine The therapeutic efficacy of Sotorasib can be decreased when used in combination with Lafutidine.
Lavoltidine The therapeutic efficacy of Sotorasib can be decreased when used in combination with Lavoltidine.
Niperotidine The therapeutic efficacy of Sotorasib can be decreased when used in combination with Niperotidine.
Aluminium The therapeutic efficacy of Sotorasib can be decreased when used in combination with Aluminium.
Magnesium oxide The therapeutic efficacy of Sotorasib can be decreased when used in combination with Magnesium oxide.
Sodium bicarbonate The therapeutic efficacy of Sotorasib can be decreased when used in combination with Sodium bicarbonate.
Aluminum hydroxide The therapeutic efficacy of Sotorasib can be decreased when used in combination with Aluminum hydroxide.
Calcium carbonate The therapeutic efficacy of Sotorasib can be decreased when used in combination with Calcium carbonate.
Magaldrate The therapeutic efficacy of Sotorasib can be decreased when used in combination with Magaldrate.
Magnesium hydroxide The therapeutic efficacy of Sotorasib can be decreased when used in combination with Magnesium hydroxide.
Magnesium trisilicate The therapeutic efficacy of Sotorasib can be decreased when used in combination with Magnesium trisilicate.
Magnesium carbonate The therapeutic efficacy of Sotorasib can be decreased when used in combination with Magnesium carbonate.
Bismuth subnitrate The therapeutic efficacy of Sotorasib can be decreased when used in combination with Bismuth subnitrate.
Magnesium silicate The therapeutic efficacy of Sotorasib can be decreased when used in combination with Magnesium silicate.
Aluminium acetoacetate The therapeutic efficacy of Sotorasib can be decreased when used in combination with Aluminium acetoacetate.
Hydrotalcite The therapeutic efficacy of Sotorasib can be decreased when used in combination with Hydrotalcite.
Magnesium peroxide The therapeutic efficacy of Sotorasib can be decreased when used in combination with Magnesium peroxide.
Almasilate The therapeutic efficacy of Sotorasib can be decreased when used in combination with Almasilate.
Aluminium glycinate The therapeutic efficacy of Sotorasib can be decreased when used in combination with Aluminium glycinate.
Aloglutamol The therapeutic efficacy of Sotorasib can be decreased when used in combination with Aloglutamol.
Calcium silicate The therapeutic efficacy of Sotorasib can be decreased when used in combination with Calcium silicate.
Aluminium phosphate The therapeutic efficacy of Sotorasib can be decreased when used in combination with Aluminium phosphate.
Phenytoin The serum concentration of Sotorasib can be decreased when it is combined with Phenytoin.
Pentobarbital The serum concentration of Sotorasib can be decreased when it is combined with Pentobarbital.
Carbamazepine The serum concentration of Sotorasib can be decreased when it is combined with Carbamazepine.
Mitotane The serum concentration of Sotorasib can be decreased when it is combined with Mitotane.
Primidone The serum concentration of Sotorasib can be decreased when it is combined with Primidone.
Rimexolone The serum concentration of Sotorasib can be decreased when it is combined with Rimexolone.
Rifampin The serum concentration of Sotorasib can be decreased when it is combined with Rifampicin.
Phenobarbital The serum concentration of Sotorasib can be decreased when it is combined with Phenobarbital.
Rifapentine The serum concentration of Sotorasib can be decreased when it is combined with Rifapentine.
Dexamethasone The serum concentration of Sotorasib can be decreased when it is combined with Dexamethasone.
Fosphenytoin The serum concentration of Sotorasib can be decreased when it is combined with Fosphenytoin.
St. John's Wort The serum concentration of Sotorasib can be decreased when it is combined with St. John's Wort.
Midostaurin The serum concentration of Sotorasib can be decreased when it is combined with Midostaurin.
Enzalutamide The serum concentration of Sotorasib can be decreased when it is combined with Enzalutamide.
Lumacaftor The serum concentration of Sotorasib can be decreased when it is combined with Lumacaftor.
Apalutamide The serum concentration of Sotorasib can be decreased when it is combined with Apalutamide.
Calcitriol The serum concentration of Calcitriol can be decreased when it is combined with Sotorasib.
Vitamin E The serum concentration of Vitamin E can be decreased when it is combined with Sotorasib.
Cholecalciferol The serum concentration of Cholecalciferol can be decreased when it is combined with Sotorasib.
Fluvoxamine The serum concentration of Fluvoxamine can be decreased when it is combined with Sotorasib.
Flunisolide The serum concentration of Flunisolide can be decreased when it is combined with Sotorasib.
Cevimeline The serum concentration of Cevimeline can be decreased when it is combined with Sotorasib.
Phentermine The serum concentration of Phentermine can be decreased when it is combined with Sotorasib.
Tramadol The serum concentration of Tramadol can be decreased when it is combined with Sotorasib.
Erythromycin The serum concentration of Erythromycin can be decreased when it is combined with Sotorasib.
Sildenafil The serum concentration of Sildenafil can be decreased when it is combined with Sotorasib.
Azithromycin The serum concentration of Azithromycin can be decreased when it is combined with Sotorasib.
Citalopram The serum concentration of Citalopram can be decreased when it is combined with Sotorasib.
Eletriptan The serum concentration of Eletriptan can be decreased when it is combined with Sotorasib.
Nelfinavir The serum concentration of Nelfinavir can be decreased when it is combined with Sotorasib.
Indinavir The serum concentration of Indinavir can be decreased when it is combined with Sotorasib.
Lovastatin The serum concentration of Lovastatin can be decreased when it is combined with Sotorasib.
Reboxetine The serum concentration of Reboxetine can be decreased when it is combined with Sotorasib.
Nevirapine The serum concentration of Nevirapine can be decreased when it is combined with Sotorasib.
Alclometasone The serum concentration of Alclometasone can be decreased when it is combined with Sotorasib.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Sotorasib.
Ziprasidone The serum concentration of Ziprasidone can be decreased when it is combined with Sotorasib.
Methysergide The serum concentration of Methysergide can be decreased when it is combined with Sotorasib.
Dapsone The serum concentration of Dapsone can be decreased when it is combined with Sotorasib.
Medrysone The serum concentration of Medrysone can be decreased when it is combined with Sotorasib.
Diethylstilbestrol The serum concentration of Diethylstilbestrol can be decreased when it is combined with Sotorasib.
Isradipine The serum concentration of Isradipine can be decreased when it is combined with Sotorasib.
Disopyramide The serum concentration of Disopyramide can be decreased when it is combined with Sotorasib.
Lidocaine The serum concentration of Lidocaine can be decreased when it is combined with Sotorasib.
Venlafaxine The serum concentration of Venlafaxine can be decreased when it is combined with Sotorasib.
Conjugated estrogens The serum concentration of Conjugated estrogens can be decreased when it is combined with Sotorasib.
Amcinonide The serum concentration of Amcinonide can be decreased when it is combined with Sotorasib.
Etonogestrel The serum concentration of Etonogestrel can be decreased when it is combined with Sotorasib.
Morphine The serum concentration of Morphine can be decreased when it is combined with Sotorasib.
Bupivacaine The serum concentration of Bupivacaine can be decreased when it is combined with Sotorasib.
Desogestrel The serum concentration of Desogestrel can be decreased when it is combined with Sotorasib.
Bexarotene The serum concentration of Bexarotene can be decreased when it is combined with Sotorasib.
Acetaminophen The serum concentration of Acetaminophen can be decreased when it is combined with Sotorasib.
Gefitinib The serum concentration of Gefitinib can be decreased when it is combined with Sotorasib.
Codeine The serum concentration of Codeine can be decreased when it is combined with Sotorasib.
Amitriptyline The serum concentration of Amitriptyline can be decreased when it is combined with Sotorasib.
Fluorometholone The serum concentration of Fluorometholone can be decreased when it is combined with Sotorasib.
Methadone The serum concentration of Methadone can be decreased when it is combined with Sotorasib.

Target Protein

GTPase KRas KRAS

Referensi & Sumber

Artikel (PubMed)
  • PMID: 31189530
    Authors unspecified: AMG 510 First to Inhibit "Undruggable" KRAS. Cancer Discov. 2019 Aug;9(8):988-989. doi: 10.1158/2159-8290.CD-NB2019-073. Epub 2019 Jun 12.
  • PMID: 23313110
    Fiala O, Pesek M, Finek J, Benesova L, Belsanova B, Minarik M: The dominant role of G12C over other KRAS mutation types in the negative prediction of efficacy of epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer. Cancer Genet. 2013 Jan-Feb;206(1-2):26-31. doi: 10.1016/j.cancergen.2012.12.003. Epub 2013 Jan 10.
  • PMID: 31666701
    Canon J, Rex K, Saiki AY, Mohr C, Cooke K, Bagal D, Gaida K, Holt T, Knutson CG, Koppada N, Lanman BA, Werner J, Rapaport AS, San Miguel T, Ortiz R, Osgood T, Sun JR, Zhu X, McCarter JD, Volak LP, Houk BE, Fakih MG, O'Neil BH, Price TJ, Falchook GS, Desai J, Kuo J, Govindan R, Hong DS, Ouyang W, Henary H, Arvedson T, Cee VJ, Lipford JR: The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity. Nature. 2019 Oct 30. pii: 10.1038/s41586-019-1694-1. doi: 10.1038/s41586-019-1694-1.
  • PMID: 31658955
    Christensen JG, Hallin J, Engstrom LD, Hargis L, Calinisan A, Aranda R, Briere DM, Sudhakar N, Bowcut V, Baer BR, Ballard JA, Burkard MR, Fell JB, Fischer JP, Vigers GP, Xue JY, Gatto S, Fernandez-Banet J, Pavlicek A, Velastegui K, Chao RC, Barton J, Pierobon M, Baldelli E, Patricoin EF, Cassidy DP, Marx MA, Rybkin II, Johnson ML, Ou SI, Lito P, Papadopoulos KP, Janne PA, Olson P: The KRASG12C Inhibitor, MRTX849, Provides Insight Toward Therapeutic Susceptibility of KRAS Mutant Cancers in Mouse Models and Patients. Cancer Discov. 2019 Oct 28. pii: 2159-8290.CD-19-1167. doi: 10.1158/2159-8290.CD-19-1167.
  • PMID: 32955176
    Hong DS, Fakih MG, Strickler JH, Desai J, Durm GA, Shapiro GI, Falchook GS, Price TJ, Sacher A, Denlinger CS, Bang YJ, Dy GK, Krauss JC, Kuboki Y, Kuo JC, Coveler AL, Park K, Kim TW, Barlesi F, Munster PN, Ramalingam SS, Burns TF, Meric-Bernstam F, Henary H, Ngang J, Ngarmchamnanrith G, Kim J, Houk BE, Canon J, Lipford JR, Friberg G, Lito P, Govindan R, Li BT: KRAS(G12C) Inhibition with Sotorasib in Advanced Solid Tumors. N Engl J Med. 2020 Sep 24;383(13):1207-1217. doi: 10.1056/NEJMoa1917239. Epub 2020 Sep 20.

Contoh Produk & Brand

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International Brands
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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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