122111-03-9

Description

Gemcitabine HCl is a synthetic difluoro nucleoside drug with anti-metabolic and antineoplastic properties. It was developed by Eli Lilly and Company and approved for clinical use in various countries, including the United States, for the treatment of non-small cell lung cancer (NSCLC) and pancreatic cancer.

Researched and developed by Eli Lilly and Company.
Approved for clinical use in South Africa, Sweden, the Netherlands, Australia, and other countries in 1995.
FDA approved Gemcitabine HCl as the first-line therapy for non-small cell lung cancer and pancreatic cancer.

Distinguish

1.Take appropriate amount of gemcitabine hydrochloride, make into solution containing the 10μg per ml by adding water and measure it according to the spectrophotometric method (Chinese Pharmacopoeia Edition 2000 Part 2 Appendix Ⅳ A). It has the maximum absorption at the wavelength of 269nm, and the minimum absorption at the wavelength of 249nm. 2.In the chromatogram recorded in content determination, the retention time of the major peak in the test solution should correspond to that in the reference solution. 3.The infrared absorption spectrum should be consistent with the reference standard spectrum. 4.Identification reaction that aqueous solution is chloride. (Chinese Pharmacopoeia Edition 2000 Part two Appendix III)

Adverse reactions and side effects

The effect of bone marrow suppression. Symptoms such as anemia, leucopenia and thrombocytopenia will appear. Approximately 66% of patients have liver aminotransferase abnormalities, which mostly are mild, non-progressive damage. About 33% of patients experience nausea and vomiting. About 50% of patients have the symptoms of mild proteinuria and hematuria. There are some cases of unexplained renal failure. About 25% of patients have skin rash, 10% patients with itching. Less than 1% of patients experience bronchial spasms. Gemcitabine hydrochloride has significant cytotoxic activity on cultured human and mouse tumors, whose antitumor activity is associated with the administration. For example, daily dosing can lead to death of the animal, but the anti-cancer activity is very small; and when giving the drug every 3-4 days at a time, drug dose is non-lethal dose and has good anti-tumor activities on many tumors.

Main manufacturers of Gemcitabine HCl include Jiangsu Stock hausen Pharmaceutical Co., Ltd., and Harbin Yu Heng Pharmaceutical Company.

Gemcitabine HCl is a pro-drug that undergoes phosphorylation intracellularly to form metabolites such as gemcitabine mono-phosphate (dFdCMP), gemcitabine diphosphate (dFdCDP), and gemcitabine triphosphate (dFdCTP), with the latter two being active products.
It is a nucleoside analog that plays a major role in the S phase of the cell cycle, inhibiting DNA synthesis and exhibiting anti-cancer activity, particularly in non-small cell lung cancer.

Chemical Properties

White crystalline granular, odorless

Originator

Lilly (U.S.A.)

Definition

ChEBI: A 2'-deoxycytidine hydrochloriode having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine hydrochloride is used in the treatment of various carcinomas, including non-small cell lung cancer, pancreatic ca cer, bladder cancer and breast cancer.

Brand name

Gemzar (Lilly).

Biological Activity

Deoxycytidine analog that inhibits DNA synthesis. Metabolized to form gemcitabine triphosphate (dFdCTP) and gemcitabine diphosphate (dFdCDP). dFdCTD inhibits ribonucleotide reductase causing a reduction in cellular nucleotides. dFdCTP is incorporated in DNA resulting in DNA strand termination. Displays antitumor activity in vitro and in vivo .