Detail of "153212-75-0"

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New in vitro metabolites of paclitaxel in humans, rats, minipigs and regular pigs

New in vitro metabolites of paclitaxel in humans, rats, minipigs and regular pigs. Vaclavikova, R.; Horsky, S.; Gut, I. (Center of Occupational Diseases, National Institute of Public Health, Prague, Czech Rep.). Cytochromes P450: Biochemistry, Biophysics and Drug Metabolism, International Conference on Cytochromes P450, 13th, Prague, Czech Republic, June 29-July 3, 2003, Meeting Date 2003, 323-326. Edited by: Anzenbacher, Pavel; Hudecek, Jiri. Monduzzi Editore: Bologna, Italy. ISBN: 88-323-3142-X(English) 2003. CODEN: 69FTSZ. DOCUMENT TYPE: Conference; (computer optical disk) CA Section: 1 (Pharmacology) We investigated in vitro interspecies variability in the metab. of important anticancer drug paclitaxel. In the rat microsomes, paclitaxel was metabolized mainly to C3'-hydroxypaclitaxel (C3'-OHP), C2-hydroxypaclitaxel (C2-OHP), di-hydroxypaclitaxel (di-OHP) and an unknown hydroxypaclitaxel.In this experiment, several chemicals are used like 33069-62-4 and 153212-75-0 In the minipig microsomes, this unknown hydroxypaclitaxel was the main metabolite, whereas C3'-OHP and C2-OHP were minor products; in the regular pig microsomes, the same metabolic pattern was demonstrated. In human liver microsomes 6a-hydroxypaclitaxel (6a-OHP) was the main metabolite, followed by C3'OHP, C2-OHP and two other metabolites not yet fully characterized. .

Pharmacokinetics of paclitaxel and carboplatin in a dose escalating and dose sequencing study in patients with non small cell lung cancer

Pharmacokinetics of paclitaxel and carboplatin in a dose escalating and dose sequencing study in patients with non small cell lung cancer. Huizing, Manon T.; Giaccone, Giuseppe; Van Warmerdam, Laurence J.Several substances are used for example 41575-94-4 and 153212-75-0 which are their cas registry numbers. C.; Rosing, Hilde; Bakker, Piet J. M.; Vermorken, Jan B.; Postmus, Piet E.; van Zandwijk, Nico; Van Koolen, Mia G. J.; et al. (Department of Medical Oncology and Pulmonology, Free University Hospital, Amsterdam, Neth.). Journal of Clinical Oncology, 15(1), 317-329 (English) 1997 Saunders. CODEN: JCONDN. ISSN: 0732-183X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The aim of our study was to investigate the pharmacokinetics and pharmacodynamics of paclitaxel (P) and carboplatin (C) in a sequence-finding and dose-escalating study in untreated non-small-cell lung cancer (NSCLC) patients. Fifty-five chemotherapy-naive patients with NSCLC were entered onto the pharmacokinetic part of a large phase 1 trial in which P was administered as a 3-h infusion at dosages of 100 to 250 mg/ m2, and C over 30 min at dosages of 300 to 400 mg/m2. Patients were randomized for the sequence of administration, first C followed by P or vice versa. Each patient received the alternate sequence during the second and subsequent courses. The most important hematol. toxicity encountered was neutropenia. Hematol. toxicity was not dependent on the sequence in which P and C were administered, but there was cumulative neutropenia. Nonhematol. toxicities consisted mainly of vomiting, myalgia, and arthralgia. No sequence-dependent pharmacokinetic interactions for the P area under the concn.-time curve (P-AUC), maximal plasma concn. (P-Cmax), or time above a threshold concn. of 0.1mmol/L (P-T 3 0.1 mmol/L) were obsd. However, there was a significant difference for the metabolite 6a-hydroxypaclitaxel AUC (60HP-AUC). Higher 60HP-AUCs were obsd. when C was administered before P. The mean plasma ultrafiltrate AUC of C (CpUF-AUC) at the dosage of 300 mg/m2 for the sequence C ? P was 3.52 mg/mL - min (range, 1.94 to 5.83) and 3.62 mg/mL - min for the sequence P ? C (range, 1.91 to 5.01), which is not significantly different (P = .55). Of 45 assessable patients, there were five major responders (three complete responders and two partial responders). Four of five responses occurred at dosages above dose level 4 (P 175 mg/m2 + C 300 mg/m2). The median survival duration was best correlated with the P dose (4.8 mo for doses < 175 mg/m2 v 7.9 mo for doses 3 175 mg/m2, P = .07; P-T 3 0.1 mmol/L, 4.8 mo for < 15 h v 8.2 mo for 3 15 h, P = .06). There was no pharmacokinetic-sequence interaction between C and P in this study. A clear dose-response relation with respect to response rate and survival was obsd. The pharmacokinetic parameter P-T 3 0.1 mmol/L was related to improved survival in this study. .