Coadministration of rifampin significantly reduces odanacatib concentrations in healthy subjects
SA Stoch, J Ballard, C Gibson… - The Journal of …, 2017 - Wiley Online Library
This open‐label 2‐period study assessed the effect of multiple‐dose administration of
rifampin, a strong cytochrome P450 3A (CYP3A) and P‐glycoprotein inducer, on the …
rifampin, a strong cytochrome P450 3A (CYP3A) and P‐glycoprotein inducer, on the …
Association between clinically relevant toxicities of pazopanib and sunitinib and the use of weak CYP3A4 and P-gp inhibitors
C Azam, P Claraz, C Chevreau, C Vinson… - European Journal of …, 2020 - Springer
Purpose Sunitinib and pazopanib, two tyrosine kinase inhibitors (TKI), may be targets of
potential pharmacokinetic drug-drug interactions (P-PK-DDIs). While strong cytochrome …
potential pharmacokinetic drug-drug interactions (P-PK-DDIs). While strong cytochrome …
ABCB1 and ABCG2 control brain accumulation and intestinal disposition of the novel ROS1/TRK/ALK inhibitor Repotrectinib, while OATP1A/1B, ABCG2, and CYP3A …
W Li, RW Sparidans, MC Lebre, JH Beijnen… - Pharmaceutics, 2021 - mdpi.com
Repotrectinib shows high activity against ROS1/TRK/ALK fusion-positive cancers in
preclinical studies. We explored the roles of multidrug efflux transporters ABCB1 and …
preclinical studies. We explored the roles of multidrug efflux transporters ABCB1 and …
Contributions of UDP-glucuronosyltransferases to human hepatic and intestinal metabolism of ticagrelor and inhibition of UGTs and cytochrome P450 enzymes by …
S Liu, L Hou, C Li, Y Zhao, X Yao, X Zhang… - Frontiers in …, 2021 - frontiersin.org
Ticagrelor is the first reversibly binding, direct-acting, oral P2Y12 receptor inhibitor. The
contribution of UDP-glucuronosyltransferases (UGTs) enzymes to the metabolism of …
contribution of UDP-glucuronosyltransferases (UGTs) enzymes to the metabolism of …
Pharmacokinetics, pharmacodynamics, tolerability and safety of single ascending doses of ticagrelor, a reversibly binding oral P2Y12 receptor antagonist, in healthy …
R Teng, K Butler - European journal of clinical pharmacology, 2010 - Springer
Purpose Ticagrelor (AZD6140) is the first reversibly binding oral P2Y 12 receptor antagonist
in development for reduction of clinical thrombotic events in patients with acute coronary …
in development for reduction of clinical thrombotic events in patients with acute coronary …
Exposure–response analysis of efficacy and safety for pexidartinib in patients with tenosynovial giant cell tumor
O Yin, H Zahir, J French, D Polhamus… - CPT …, 2021 - Wiley Online Library
This analysis was conducted to assess exposure–response relationships for efficacy and
safety of pexidartinib in patients with tenosynovial giant cell tumor. Efficacy was assessed …
safety of pexidartinib in patients with tenosynovial giant cell tumor. Efficacy was assessed …
Influence of mild and moderate hepatic impairment on the pharmacokinetics (PK) of the pan-HER inhibitor dacomitinib.
N Giri, A Plotka, Y Liang, T Boutros, G Ni, J Masters… - 2013 - ascopubs.org
2568 Background: Dacomitinib (D) is a highly selective irreversible small molecule inhibitor
of the HER family of tyrosine kinases in clinical development for NSCLC. Prior clinical …
of the HER family of tyrosine kinases in clinical development for NSCLC. Prior clinical …
Preclinical assessment of ulixertinib, a novel ERK1/2 inhibitor
VA Balakrishna, A Police, RA Hiremath, A Raj… - ADMET and …, 2017 - hrcak.srce.hr
Sažetak Ulixertinib (BVD-523) is a novel and selective reversible inhibitor of ERK1/ERK2. In
xenograft studies it inhibited tumor growth in BRAF-mutant melanoma and colorectal …
xenograft studies it inhibited tumor growth in BRAF-mutant melanoma and colorectal …
Increased bioavailability of intravenous versus oral CI-1033, a pan erbB tyrosine kinase inhibitor: results of a phase I pharmacokinetic study
GR Simon, CR Garrett, SC Olson, M Langevin… - Clinical cancer …, 2006 - AACR
Purpose: In phase I studies with oral CI-1033, dose-limiting toxicities were primarily
gastrointestinal, supporting the exploration of iv dosing to achieve optimal drug exposures …
gastrointestinal, supporting the exploration of iv dosing to achieve optimal drug exposures …
Evaluation of ipatasertib interactions with itraconazole and coproporphyrin I and III in a single drug interaction study in healthy subjects
RS Sane, KWK Cheung, E Cho, BM Liederer… - … of Pharmacology and …, 2021 - ASPET
Ipatasertib is a pan-AKT inhibitor in development for the treatment of cancer. Ipatasertib was
metabolized by CYP3A4 to its major metabolite, M1 (G-037720), and was a P-gp substrate …
metabolized by CYP3A4 to its major metabolite, M1 (G-037720), and was a P-gp substrate …