دورية أكاديمية
Effect of Strong CYP3A4 Inhibition, CYP3A4 Induction, and OATP1B1/3 Inhibition on the Pharmacokinetics of a Single Oral Dose of Sotorasib.
| العنوان: | Effect of Strong CYP3A4 Inhibition, CYP3A4 Induction, and OATP1B1/3 Inhibition on the Pharmacokinetics of a Single Oral Dose of Sotorasib. |
|---|---|
| المؤلفون: | Cardona P; Clinical Pharmacology, Modeling and Simulation, Amgen Inc., Thousand Oaks, CA, USA., Dutta S; Clinical Pharmacology, Modeling and Simulation, Amgen Inc., Thousand Oaks, CA, USA., Houk B; Clinical Pharmacology, Modeling and Simulation, Amgen Inc., Thousand Oaks, CA, USA. |
| المصدر: | Clinical pharmacology in drug development [Clin Pharmacol Drug Dev] 2024 Jul; Vol. 13 (7), pp. 810-818. Date of Electronic Publication: 2024 Feb 29. |
| نوع المنشور: | Journal Article; Clinical Trial, Phase I; Randomized Controlled Trial |
| اللغة: | English |
| بيانات الدورية: | Publisher: Wiley Country of Publication: United States NLM ID: 101572899 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 2160-7648 (Electronic) Linking ISSN: 2160763X NLM ISO Abbreviation: Clin Pharmacol Drug Dev Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: 2013- : Hoboken, NJ : Wiley Original Publication: Thousand Oaks, Calif. : Sage Publications, c2012- |
| مواضيع طبية MeSH: | Liver-Specific Organic Anion Transporter 1*/antagonists & inhibitors , Liver-Specific Organic Anion Transporter 1*/metabolism , Solute Carrier Organic Anion Transporter Family Member 1B3*/antagonists & inhibitors , Solute Carrier Organic Anion Transporter Family Member 1B3*/metabolism , Cytochrome P-450 CYP3A Inhibitors*/pharmacology , Cytochrome P-450 CYP3A Inhibitors*/administration & dosage , Cytochrome P-450 CYP3A*/metabolism , Rifampin*/pharmacology , Rifampin*/administration & dosage , Drug Interactions* , Cytochrome P-450 CYP3A Inducers*/pharmacology, Humans ; Male ; Adult ; Female ; Young Adult ; Administration, Oral ; Middle Aged ; Healthy Volunteers ; Area Under Curve ; Itraconazole/pharmacology ; Itraconazole/administration & dosage ; Itraconazole/pharmacokinetics ; Spiro Compounds/pharmacokinetics ; Spiro Compounds/administration & dosage ; Spiro Compounds/pharmacology |
| مستخلص: | Sotorasib is a small molecule that irreversibly inhibits the Kirsten rat sarcoma viral oncogene homolog (KRAS) protein with a G12C amino acid substitution mutant protein. The impact of cytochrome P450 (CYP) 3A4 inhibition and induction on sotorasib pharmacokinetics (PKs) was evaluated in 2 separate studies in healthy volunteers (N = 14/study). The impact of CYP3A4 inhibition was interrogated utilizing repeat doses of 200 mg of itraconazole, a strong CYP3A4 inhibitor, on 360 mg of sotorasib PKs. The impact of CYP3A4 induction was interrogated utilizing multiple doses of 600 mg of rifampin, a strong CYP3A4 inducer. Additionally, the impact of organic anion transporting polypeptide (OATP) 1B1/3 inhibition on 960 mg of sotorasib PKs was interrogated after a single dose of 600 mg of rifampin. CYP3A4 inhibition did not significantly impact sotorasib C (© 2024, The American College of Clinical Pharmacology.) |
| References: | Ostrem JM, Shokat KM. Direct small‐molecule inhibitors of KRAS: from structural insights to mechanism‐based design. Nat Rev Drug Discov. 2016;15(11):771‐785. Biernacka A, Tsongalis PD, Peterson JD, et al. The potential utility of re‐mining results of somatic mutation testing: KRAS status in lung adenocarcinoma. Cancer Genet. 2016;209(5):195‐198. Neumann, J., Zeindl‐Eberhart E, Kirchner T, Jung A. Frequency and type of KRAS mutations in routine diagnostic analysis of metastatic colorectal cancer. Pathol Res Pract. 2009;205(12):858‐862. Vuu I, Wahlstrom J, Houk BE. Impact of sotorasib on the pharmacokinetics and pharmacodynamics of metformin, a MATE1/2K substrate, in healthy subjects. Clin Pharmacokinet. 2023;62(2):267‐275. Vuu I, Dahal UP, Wang Z, et al. Absorption, metabolism and excretion of [(14)C]‐sotorasib in healthy male subjects: characterization of metabolites and a minor albumin‐sotorasib conjugate. Cancer Chemother Pharmacol. 2022;90(4):357‐367. Banankhah PS, Garnick KA, Greenblatt DJ. Ketoconazole‐associated liver injury in drug‐drug interaction studies in healthy volunteers. J Clin Pharmacol. 2016;56(10):1196‐1202. Greenblatt DJ. Evidence‐based choice of ritonavir as index CYP3A inhibitor in drug‐drug interaction studies. J Clin Pharmacol. 2016;56(2):152‐156. Greenblatt DJ, Harmatz JS. Ritonavir is the best alternative to ketoconazole as an index inhibitor of cytochrome P450‐3A in drug‐drug interaction studies. Br J Clin Pharmacol. 2015;80(3):342‐350. Greenblatt DJ, Mikus G. Ketoconazole and liver injury: a five‐year update. Clin Pharmacol Drug Dev. 2019;8(1):6‐8. Outeiro N, Hohmann N, Mikus G. No increased risk of ketoconazole toxicity in drug‐drug interaction studies. J Clin Pharmacol. 2016;56(10):1203‐1211. Templeton I, Peng CC, Thummel KE, Davis C, Kunze KL. Accurate prediction of dose‐dependent CYP3A4 inhibition by itraconazole and its metabolites from in vitro inhibition data. Clin Pharmacol Ther. 2010;88(4):499‐505. Backman, JT, Kivistö KT, Olkkola KT, Neuvonen PJ. The area under the plasma concentration‐time curve for oral midazolam is 400‐fold larger during treatment with itraconazole than with rifampicin. Eur J Clin Pharmacol. 1998;54(1):53‐58. Olkkola KT, Ahonen J, Neuvonen PJ. The effects of the systemic antimycotics, itraconazole and fluconazole, on the pharmacokinetics and pharmacodynamics of intravenous and oral midazolam. Anesth Analg. 1996;82(3):511‐516. Kivisto KT, Kantola T, Neuvonen PJ. Different effects of itraconazole on the pharmacokinetics of fluvastatin and lovastatin. Br J Clin Pharmacol. 1998;46(1):49‐53. Jalava KM, Olkkola KT, Neuvonen PJ. Itraconazole greatly increases plasma concentrations and effects of felodipine. Clin Pharmacol Ther. 1997;61(4):410‐415. Liu L, Bello A, Dresser MJ, et al. Best practices for the use of itraconazole as a replacement for ketoconazole in drug‐drug interaction studies. J Clin Pharmacol. 2016;56(2):143‐151. Choi MK, Jin QR, Choi YL, Ahn SH, Bae MA, Song IS. Inhibitory effects of ketoconazole and rifampin on OAT1 and OATP1B1 transport activities: considerations on drug‐drug interactions. Biopharm Drug Dispos. 2011;32(3):175‐184. Chen J, Raymond K. Roles of rifampicin in drug‐drug interactions: underlying molecular mechanisms involving the nuclear pregnane X receptor. Ann Clin Microbiol Antimicrob. 2006;5:3. Kapetas AJ, Sorich MJ, Rodrigues AD, Rowland A, Guidance for rifampin and midazolam dosing protocols to study intestinal and hepatic cytochrome P450 (CYP) 3A4 induction and de‐induction. AAPS J. 2019;21(5):78. Wong P, Akrami A, Houk B, Vuu I, James CA. Validation of an LC‐MS/MS method for the determination of sotorasib, a KRAS(G12C) inhibitor, in human plasma. Bioanalysis. 2022;14(19):1281‐1292. FDA. Guidance for Industry Clinical Drug Interaction Studies – Cytochrome P450 Enzyme‐ and Transporter‐Mediated Drug Interactions. 2020. von Richter O, Burk O, Fromm MF, Thon KP, Cytochrome P450 3A4 and P‐glycoprotein expression in human small intestinal enterocytes and hepatocytes: a comparative analysis in paired tissue specimens. Clin Pharmacol Ther. 2004;75(3):172‐183. Baneyx G, Parrott N, Meille C, Iliadis A, Lavé T. Physiologically based pharmacokinetic modeling of CYP3A4 induction by rifampicin in human: influence of time between substrate and inducer administration. Eur J Pharm Sci. 2014;56:1‐15. Kajosaari, LI, Laitila J, Neuvonen PJ, Backman JT, Metabolism of repaglinide by CYP2C8 and CYP3A4 in vitro: effect of fibrates and rifampicin. Basic Clin Pharmacol Toxicol. 2005;97(4):249‐256. |
| فهرسة مساهمة: | Keywords: CYP3A4; KRAS inhibitor; drug interaction; oncology; sotorasib |
| المشرفين على المادة: | 0 (Liver-Specific Organic Anion Transporter 1) 0 (SLCO1B1 protein, human) 0 (Solute Carrier Organic Anion Transporter Family Member 1B3) 0 (Cytochrome P-450 CYP3A Inhibitors) 0 (SLCO1B3 protein, human) EC 1.14.14.1 (Cytochrome P-450 CYP3A) VJT6J7R4TR (Rifampin) 0 (Cytochrome P-450 CYP3A Inducers) EC 1.14.14.55 (CYP3A4 protein, human) 304NUG5GF4 (Itraconazole) 0 (Spiro Compounds) |
| تواريخ الأحداث: | Date Created: 20240229 Date Completed: 20240703 Latest Revision: 20240703 |
| رمز التحديث: | 20240704 |
| DOI: | 10.1002/cpdd.1392 |
| PMID: | 38421129 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 2160-7648 |
|---|---|
| DOI: | 10.1002/cpdd.1392 |