Zalcitabine. Clinical pharmacokinetics and efficacy.

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Devineni D, Gallo JM

Zalcitabine. Clinical pharmacokinetics and efficacy.

Clin Pharmacokinet. 1995 May;28(5):351-60.

PubMed ID

7614775 [ View in PubMed

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Abstract

Zalcitabine (ddC) was the first drug to be approved under the US Food and Drug Administration's (FDA's) accelerated drug approval process. Zalcitabine is a potent nucleoside analogue inhibitor of reverse transcriptase used in the treatment of HIV infection. It is approximately 10-fold more potent than zidovudine (AZT) on a molar basis in vitro. Zalcitabine is well absorbed orally and reaches maximal plasma concentrations within 1 to 2 hours. In humans it is mainly eliminated by renal excretion of unchanged drug, and patients with renal failure may exhibit a prolonged half-life. A variety of clinical trials have evaluated the efficacy of zalcitabine based on improved survival and decreased frequency of opportunistic infections and on a surrogate marker of HIV disease, the CD4 count, or the concentration of an antigen associated with HIV, p24. Alternating zalcitabine therapy with zidovudine therapy was associated with increased CD4+ lymphocyte counts and reduced plasma p24 antigen levels. Zalcitabine can cause peripheral neuropathy (in 17 to 31% of patients), which is dose-related and is completely reversible when the drug is discontinued. Zalcitabine will continue to play a role in chemotherapeutic approaches to HIV.

DrugBank Data that Cites this Article

Drugs

Zalcitabine

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Zalcitabine	Reverse transcriptase/RNaseH	Protein	Human immunodeficiency virus 1	Yes	Inhibitor	Details