2021 DECEMBER

Species differences

Drug Metab Dispos. 2021;In press. Mechanistic study on the species differences in excretion pathway of HR011303 in human and rats. Guo Z, Liu M, Meng J, Xue Y, Huang Q, Zheng Y, Wu Y, Chen Z, Yu J, Zhong D, Li G, Chen X, Diao X. PubMed

Drug Metab Pharmacokinet. 2021;41:100418. Differences in transport function of the human and rat orthologue of the Organic Anion Transporting Polypeptide 2B1 (OATP2B1). Hussner J, Foletti A, Seibert I, Fuchs A, Schuler E, Malagnino V, Grube M, Meyer Zu Schwabedissen HE. PubMed

NTCP and HBV

Mol Ther Methods Clin Dev;In press. Genetically edited hepatic cells expressing the NTCP-S267F variant are resistant to hepatitis B virus infection. Uchida T, Park SB, Inuzuka T, Zhang M, Allen JN, Chayama K, Liang TJ. PubMed

Hepatotoxicity

Mol Nutr Food Res. 2021;In press. Organic Cation Transporter I and Na⁺/taurocholate Co-Transporting Polypeptide are involved in Retrorsine- and Senecionine-induced hepatotoxicity in HepaRG cells.  Enge AM, Kaltner F, Gottschalk C, Kin A, Kirstgen M, Geyer J, These A, Hammer H, Pötz O, Braeuning A, Hessel-Pras S. PubMed

J Pharmacol Exp Ther. 2021;In press. Novel bile acid-dependent mechanisms of hepatotoxicity associated with Tyrosine Kinase inhibitors. Saran C, Sundqvist L, Ho H, Niskanen J, Honkakoski P, Brouwer KL. PubMed

Transporter activities

Drug Metab Dispos. 2021;49:1109-1117. Pharmacokinetics and ADME characterization of intravenous and oral [14C]-Linerixibat in healthy male volunteers. Zamek-Gliszczynski MJ, Kenworthy D, Bershas DA, Sanghvi M, Pereira AI, Mudunuru J, Crossman L, Pirhalla JL, Thorpe KM, Dennison JMTJ, McLaughlin MM, Allinder M, Swift B, O'Connor-Semmes RL, Young GC. PubMed

Biochem Pharmacol. 2021;193:114799. Biliary excretion of arsenic by human HepaRG cells is stimulated by selenide and mediated by the multidrug resistance protein 2 (MRP2/ABCC2). Zhou JR, Kaur G, Ma Y, Arutyunov D, Lu X, Le XC, Leslie EM. PubMed

Mol Pharmacol. 2021;100:599-608. Identification of key amino acids that impact Organic Solute Transporter α/β (OSTα/β). Murphy WA, Beaudoin JJ, Laitinen T, Sjöstedt N, Malinen MM, Ho H, Swaan PW, Honkakoski P, Brouwer KLR. PubMed

Drug Metab Pharmacokinet. 2021;41:100416. Dual kinetics of OATP2B1: Inhibitory potency and pH-dependence of OATP2B1 inhibitors. Sato R, Akiyoshi T, Morita T, Katayama K, Yajima K, Kataoka H, Imaoka A, Ohtani H. PubMed

Int J Mol Sci. 2021;22:12926. Substrate-dependent Trans-Stimulation of Organic Cation Transporter 2 activity. Lefèvre CR, Le Vée M, Gaubert S, Jouan E, Bruyere A, Moreau C, Fardel O. PubMed

DDI

Pharmacol Res Perspect. 2021;9:e00870. In vitro investigations into the roles of CYP450 enzymes and drug transporters in the drug interactions of zanubrutinib, a covalent Bruton's tyrosine kinase inhibitor. Zhang H, Ou YC, Su D, Wang F, Wang L, Sahasranaman S, Tang Z. PubMed

Front Pharmacol. 2021;12:715577. Evaluation of a clinically relevant Drug-Drug Interaction between Rosuvastatin and Clopidogrel and the risk of hepatotoxicity. Ning C, Su S, Li J, Kong D, Cai H, Qin Z, Xing H, Chen X, He J. PubMed

Drug Metab Dispos. 2021;49:1063-1069. Endogenous plasma Kynurenic acid in human: A newly discovered biomarker for Drug-Drug Interactions involving Organic Anion Transporter 1 and 3 inhibition. Tang J, Shen H, Zhao X, Holenarsipur VK, Mariappan TT, Zhang Y, Panfen E, Zheng J, Humphreys WG, Lai Y. PubMed

Clin Pharmacol Ther. 2021;in press. Acute and chronic effects of Rifampin on Letermovir suggest transporter inhibition and induction contribute to Letermovir pharmacokinetics. Robbins JA, Menzel K, Lassman M, Zhao T, Fancourt C, Chu X, Mostoller K, Witter R, Marceau West R, Stoch SA, McCrea JB, Iwamoto M. PubMed

Metformin and SLC transporters

Front Endocrinol. 2021;12:720784. Restoration of mRNA expression of Solute Carrier Proteins in liver of diet-induced obese mice by Metformin. Le J, Fu Y, Han Q, Wei X, Ji H, Chen Y, Wang Q, Pi P, Li J, Lin X, Zhang X, Zhang Y, Ye J. PubMed

Bile acid transport

Clin Liver Dis (Hoboken). 2021;18:237-242. Genetic disorders of bile acid transport. Henkel AS. PubMed

Hepatic clearance

Clin Pharmacol Ther. 2021;In press. Can in vitro-in vivo extrapolation be successful? Recognizing the incorrect clearance assumptions. Benet LZ, Sodhi JK. PubMed