DHA-paclitaxel - CAS 199796-52-6
Catalog number:
199796-52-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Description:
DHA-paclitaxel, also know as Taxoprexin, is prodrug comprised of the naturally occurring omega-3 fatty acid docosahexaenoic acid (DHA) covalently conjugated to the anti-microtubule agent paclitaxel. Because tumor cells take up DHA, DHA-paclitaxel is delivered directly to tumor tissue, where the paclitaxel moiety binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. Paclitaxel also induces apoptosis by binding to and blocking the function of the apoptosis inhibitor protein Bcl-2 (B-cell Leukemia 2). DHA-paclitaxel exhibits improved pharmacokinetic and toxicity profiles when compared to conventional paclitaxel and has demonstrated antineoplastic activity in animal models of cancer.
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Synonyms:
Docosahexaenoic Acid-Paclitaxel conjugate ; Taxoprexin ,DHA-TAX; TXP; DHA-paclitaxel.
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Current Developer:
Protarga Inc
1.DHA-paclitaxel (Taxoprexin) as first-line treatment in patients with stage IIIB or IV non-small cell lung cancer: report of a phase II open-label multicenter trial.
Payne M1, Ellis P, Dunlop D, Ranson M, Danson S, Schacter L, Talbot D. J Thorac Oncol. 2006 Nov;1(9):984-90.
INTRODUCTION: This prospective, open-label, non-randomized, multi-institutional phase II study was undertaken to assess the antitumor activity and safety of docosahexaenoic acid-paclitaxel (Taxoprexin) as first-line treatment of patients with advanced non-small cell lung cancer.
2.A phase II open-label study of DHA-paclitaxel (Taxoprexin) by 2-h intravenous infusion in previously untreated patients with locally advanced or metastatic gastric or oesophageal adenocarcinoma.
Jones RJ1, Hawkins RE, Eatock MM, Ferry DR, Eskens FA, Wilke H, Evans TR. Cancer Chemother Pharmacol. 2008 Mar;61(3):435-41. Epub 2007 Apr 18.
PURPOSE: Combination chemotherapy regimens can improve survival in patients with advanced gastric and oesophageal adenocarcinoma. Docosahexaenoic acid (DHA)-paclitaxel is a novel conjugate formed by the covalent linkage of the fatty acid DHA to paclitaxel and may result in increased tumour exposure to paclitaxel without increased toxicity.
3.Phase I/II study of DHA-paclitaxel in combination with carboplatin in patients with advanced malignant solid tumours.
Harries M1, O'Donnell A, Scurr M, Reade S, Cole C, Judson I, Greystoke A, Twelves C, Kaye S. Br J Cancer. 2004 Nov 1;91(9):1651-5.
DHA-paclitaxel is a conjugate of paclitaxel and the fatty acid, docosahexaenoic acid. Preclinical studies have demonstrated increased activity, relative to paclitaxel, with the potential for an improved therapeutic ratio. We conducted a phase I study to determine the maximum tolerated doses of DHA-paclitaxel and carboplatin when administered in combination. Two cohorts of patients were treated: carboplatin AUC 5 with DHA-paclitaxel 660 mg m(-2) and carboplatin AUC 5 with DHA-paclitaxel 880 mg m(-2). Both drugs were given on day 1 every 21 days. A total of 15 patients were enrolled with a median age of 59 years (range 33-71). All patients had advanced cancer refractory to standard treatment, performance status 0-2 and were without major organ dysfunction. A total of 54 cycles of treatment were delivered. No dose-limiting toxicity (DLT) was seen in the first cohort of three patients. In an expanded second cohort, neutropenia was the main DLT, occurring in the first cycle of treatment in five of 12 patients: three of these patients and one additional patient also experienced dose-limiting grade 3 transient rises in liver transaminases.
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CAS 199796-52-6 DHA-paclitaxel

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