Zalcitabine
(7481-89-2)
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Chemistry
Zalcitabine(7481-89-2) is the chemical compound with the formula C9H13N3O3 .Its molar weight is 211.22.
Zalcitabine(7481-89-2) chemical structural formula is 
.
Synonyms : Dideoxycytidine; 2',3'-Dideoxycytidine; DDC
CAS Registry Number : 7481-89-2
Melting point : 210-214 oC
Water solubility : 5-10 g/100 mL at 19 oC
Refractive index : 78 ° (C=0.5, H2O)
Storage temp : 2-8°C
History
Zalcitabine(7481-89-2) was first synthetized in the sixties by Jerome Horwitz and subsequently developed as an anti-HIV agent by Samuel Broder, Hiroaki Mitsuya, and Robert Yarchoan at the National Cancer Institute (NCI). Like didanosine, Zalcitabine(7481-89-2) was then licensed because the NCI may not market or sell drugs. The National Institutes of Health (NIH) thus licensed it to Hoffman LaRoche.
Zalcitabine was the third antiretroviral to be approved by the Food and Drug Administration (FDA) for the treatment of HIV infection and AIDS. It was approved on Jun 19, 1992 as a monotherapy and again in 1996 for use in combination with Zidovudine (AZT). Using combinations of NRTIs was in practice prior to the second FDA approval and the triple drug combinations with dual NRTIs and a protease inhibitor (PI) were not far off by this time.
Uses
Zalcitabine(7481-89-2) appears less potent than some other nucleoside RTIs, has an inconvenient three-times daily frequency and is associated with serious adverse events. For these reasons Zalcitabine(7481-89-2) is now rarely used to treat human immunodeficiency virus (HIV), and even removed from pharmacies entirely in some countries.
Toxicity Data With Reference
| 1. |
|
dni-hmn:lym 200 nmol/L |
|
MOPMA3 Molecular Pharmacology. 39 (1991),625. |
| 2. |
|
cyt-mus-orl 600 mg/kg/3D-C |
|
EMMUEG Environmental and Molecular Mutagenesis. 18 (1991),168. |
Safety Profile
An experimental teratogen. Experimental reproductive effects. Mutation data reported.
The Hazard Codes of Zalcitabine(7481-89-2) Xn 
The Risk Statements information of Zalcitabine(7481-89-2)R63:Possible risk of harm to the unborn child.
The Safety Statements information of Zalcitabine(7481-89-2)S22:Do not inhale dust;S36/37:Wear suitable protective clothing and gloves.
