Product Name

Docetaxel

Name: Docetaxel - LGM Pharma
SKU: 114977-28-5

CAS Number

114977-28-5

LGM Pharma is an API distributor. LGM Pharma supplies APIs as per CGMP with DMF support, subject to availability and manufacturer requirements. LGM Pharma does not sell or supply APIs or finished dosage products to individual patients, doctors, or pharmacies.

Questions? Call our customer API support number 1-(800)-881-8210

Product Name:

Docetaxel

CAS Number:

114977-28-5

Indication:

For the treatment of patients with locally advanced or metastatic breast cancer after failure of prior chemotherapy. Also used as a single agent in the treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of prior platinum-based chemotherapy. Lastly, for use, in combination with prednisone, in the treatment of patients with androgen independent (hormone refractory) metastatic prostate cancer.

Mode of Action:

Docetaxel interferes with the normal function of microtubule growth. Whereas drugs like colchicine cause the depolymerization of microtubules in vivo, docetaxel arrests their function by having the opposite effect; it hyper-stabilizes their structure. This destroys the cell's ability to use its cytoskeleton in a flexible manner. Specifically, docetaxel binds to the _-subunit of tubulin. Tubulin is the "building block" of mictotubules, and the binding of docetaxel locks these building blocks in place. The resulting microtubule/docetaxel complex does not have the ability to disassemble. This adversely affects cell function because the shortening and lengthening of microtubules (termed dynamic instability) is necessary for their function as a transportation highway for the cell. Chromosomes, for example, rely upon this property of microtubules during mitosis. Further research has indicated that docetaxel induces programmed cell death (apoptosis) in cancer cells by binding to an apoptosis stopping protein called Bcl-2 (B-cell leukemia 2) and thus arresting its function.

Pharmacodynamics:

Docetaxel is a taxoid antineoplastic agent. It promotes the assembly of microtubules from tubulin dimers and stabilizes microtubules by preventing depolymerization. This stability results in the inhibition of the normal dynamic reorganization of the microtubule network that is essential for vital interphase and mitotic cellular functions. In addition, docetaxel induces abnormal arrays or "bundles" of microtubules throughout the cell cycle and multiple asters of microtubules during mitosis.

Metabolism:

Hepatic. In vitro drug interaction studies revealed that docetaxel is metabolized by the CYP3A4 isoenzyme (1 major, 3 minor metabolites).

Toxicity:

Oral LD₅₀ in rat is >2000 mg/kg. Anticipated complications of overdosage include: bone marrow suppression, peripheral neurotoxicity, and mucositis. In two reports of overdose, one patient received 150 mg/m² and the other received 200 mg/m² as 1-hour infusions. Both patients experienced severe neutropenia, mild asthenia, cutaneous reactions, and mild paresthesia, and recovered without incident.

IUPAC:

(1S, 2S, 3R, 4S, 7R, 9S, 10S, 12R, 15S)-4-(acetyloxy)-15-{[(2R, 3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-3-phenylpropanoyl]oxy}-1, 9, 12-trihydroxy-10, 14, 17, 17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.0, {3, 10}.0, {4, 7}]heptadec-13-en-2-yl benzoate

ATC:

L01CD02

PubChem:

148124

DrugBank:

DB01248 (APRD00932)

Formula:

C₃₅H₅₆N₆O₆

Molecular Mass:

807.8792

Synonyms:

Docetaxel anhydrous Docetaxel, Trihydrate TXL

SMILES:

CC(=O)O[C@@]12CO[C@@H]1C[C@H](O)[C@]1(C)[C@@H]2[C@H](OC(=O)C2=CC=CC=C2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C3=CC=CC=C3)C(C)=C([C@@H](O)C1=O)C2(C)C

AHFS Code:

10:00.0

InChi:

ZDZOTLJHXYCWBA-VCVYQWHSSA-N

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

LGM currently offers Monoclonal Antibodies (mAbs) for non-GMP/R&D use. Please inquire about Monoclonal Antibodies produced under GMP conditions.

Questions? Call our customer API support number 1-(800)-881-8210.

Ask us about this product

API’s From Quality Manufacturers:

Streamlined API supply towards initial research stages as well as larger quantities of cGMP material for clinical trials and product commercialization
Premium quality GMP certified and fully accredited API manufacturing plants
Technical packages as well as access to filed DMF, ASMF or CEP (subject to availability)
Regulatory and technical assistance towards any submission type based on specific customer requirements

Docetaxel

114977-28-5

Ask us about this product

API’s From Quality Manufacturers:

Find an API Product