ZALCITABINE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C9H13N3O3
Molecular Weight	211.2182
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

C1C[C@]([H])(n2ccc(=N)nc2O)O[C@]1([H])CO

InChI

InChIKey=WREGKURFCTUGRC-POYBYMJQSA-N

InChI=1S/C9H13N3O3/c10-7-3-4-12(9(14)11-7)8-2-1-6(5-13)15-8/h3-4,6,8,13H,1-2,5H2,(H2,10,11,14)/t6-,8+/m0/s1

HIDE SMILES / InChI

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s16lbl.pdf

The nucleoside analog 2',3'-dideoxycytidine (ddCyd), also known as Zalcitabine is a nucleoside analog reverse transcriptase inhibitor (NRTI) sold under the trade name Hivid. HIVID is indicated in combination with antiretroviral agents for the treatment of HIV infection. It is used as part of a combination regimen with antiretroviral agents. But it was discontinued by Roche Pharmaceuticals on December 31, 2006 due to the availability of newer HIV medicines. Within cells, zalcitabine is converted to the active metabolite, dideoxycytidine 5'-triphosphate (ddCTP), by the sequential action of cellular enzymes. Dideoxycytidine 5'-triphosphate inhibits the activity of the HIV-reverse transcriptase both by competing for utilization of the natural substrate, deoxycytidine 5'-triphosphate (dCTP), and by its incorporation into viral DNA. The lack of a 3'- OH group in the incorporated nucleoside analogue prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation and, therefore, the viral DNA growth is terminated. The active metabolite, ddCTP, is also an inhibitor of cellular DNA polymerasebeta and mitochondrial DNA polymerase-gamma and has been reported to be incorporated into the DNA of cells in culture.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Human immunodeficiency virus type 1 reverse transcriptase 45 Target ID: CHEMBL247 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9179531	Inhibitor 7728

Conditions

Condition	Modality	Targets	Highest Phase	Product
HIV infection 21 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s16lbl.pdf	Primary		Approved 8043	HIVID Approved Use HIVID is indicated in combination with antiretroviral agents for the treatment of HIV infection. This indication is based on study results showing a reduction in the rate of disease progression (AIDS-defining events or death) in patients with limited prior antiretroviral therapy who were treated with the combination of HIVID and zidovudine. This indication is also based on a study showing a reduction in both mortality and AIDS-defining clinical events for patients who received INVIRASE® (saquinavir mesylate) in combination with HIVID compared to patients who received either HIVID or INVIRASE alone. Launch Date 7.0891202E11

C_max

Value	Dose	Analyte	Population
7.6 μg/L REVIEW https://pubmed.ncbi.nlm.nih.gov/9179531/	0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
10.5 μg/L REVIEW https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf	0.5 mg single, intravenous dose: 0.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
79 μg/L REVIEW https://pubmed.ncbi.nlm.nih.gov/9179531/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
9.3 μg/L REVIEW https://pubmed.ncbi.nlm.nih.gov/9179531/	0.02 mg/kg bw single, oral dose: 0.02 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNHEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN
15.5 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf	1.5 mg single, oral dose: 1.5 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: FED
25.2 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf	1.5 mg single, oral dose: 1.5 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: FASTED

AUC

Value	Dose	Analyte	Population
0.018 mg × h/L REVIEW https://pubmed.ncbi.nlm.nih.gov/9179531/	0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
0.022 mg × h/L REVIEW https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf	0.5 mg single, intravenous dose: 0.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
0.208 mg × h/L REVIEW https://pubmed.ncbi.nlm.nih.gov/9179531/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
0.025 mg × h/L REVIEW https://pubmed.ncbi.nlm.nih.gov/9179531/	0.02 mg/kg bw single, oral dose: 0.02 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNHEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN
62 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf	1.5 mg single, oral dose: 1.5 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: FED
72 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf	1.5 mg single, oral dose: 1.5 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: FASTED

T_1/2

Value	Dose	Analyte	Population
1.5 h REVIEW https://pubmed.ncbi.nlm.nih.gov/9179531/	0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1.3 h REVIEW https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf	0.5 mg single, intravenous dose: 0.5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1.8 h REVIEW https://pubmed.ncbi.nlm.nih.gov/9179531/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1.4 h REVIEW https://pubmed.ncbi.nlm.nih.gov/9179531/	0.02 mg/kg bw single, oral dose: 0.02 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNHEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN
2 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf	1.5 mg single, oral dose: 1.5 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: FED
2 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf	1.5 mg single, oral dose: 1.5 mg route of administration: Oral experiment type: SINGLE co-administered:	ZALCITABINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
96% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf	1.5 mg single, oral dose: 1.5 mg route of administration: Oral experiment type: SINGLE co-administered:		ZALCITABINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: FED
96% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf	1.5 mg single, oral dose: 1.5 mg route of administration: Oral experiment type: SINGLE co-administered:		ZALCITABINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: FASTED

Doses

Dose	Population	Adverse events
0.09 mg/kg 6 times / day multiple, oral Dose: 0.09 mg/kg, 6 times / day Route: oral Route: multiple Dose: 0.09 mg/kg, 6 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/2558314 Page: p.858	unhealthy, 26-57 n = 5 Health Status: unhealthy Condition: HIV infection Age Group: 26-57 Sex: M Population Size: 5 Sources: https://pubmed.ncbi.nlm.nih.gov/2558314 Page: p.858	Disc. AE: Peripheral neuropathy, Leukopenia... AEs leading to discontinuation/dose reduction: Peripheral neuropathy (40%) Leukopenia (20%) Thrombocytopenia (40%) Sources: https://pubmed.ncbi.nlm.nih.gov/2558314 Page: p.858
0.06 mg/kg 6 times / day multiple, oral Highest studied dose Dose: 0.06 mg/kg, 6 times / day Route: oral Route: multiple Dose: 0.06 mg/kg, 6 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/2536257 Page: p.191	unhealthy, 42 n = 18 Health Status: unhealthy Condition: HIV infection Age Group: 42 Sex: M+F Population Size: 18 Sources: https://pubmed.ncbi.nlm.nih.gov/2536257 Page: p.191	Disc. AE: Peripheral neuropathy... AEs leading to discontinuation/dose reduction: Peripheral neuropathy (grade 3, 100%) Sources: https://pubmed.ncbi.nlm.nih.gov/2536257 Page: p.191
0.03 mg/kg 6 times / day multiple, oral Dose: 0.03 mg/kg, 6 times / day Route: oral Route: multiple Dose: 0.03 mg/kg, 6 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/2536257 Page: p.191	unhealthy, 42 n = 18 Health Status: unhealthy Condition: HIV infection Age Group: 42 Sex: M+F Population Size: 18 Sources: https://pubmed.ncbi.nlm.nih.gov/2536257 Page: p.191	Disc. AE: Peripheral neuropathy... AEs leading to discontinuation/dose reduction: Peripheral neuropathy (grade 3, 100%) Sources: https://pubmed.ncbi.nlm.nih.gov/2536257 Page: p.191
1.5 mg 3 times / day multiple, oral Overdose Dose: 1.5 mg, 3 times / day Route: oral Route: multiple Dose: 1.5 mg, 3 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.18	unhealthy Health Status: unhealthy Condition: HIV infection Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.18	Other AEs: Peripheral neuropathy... Other AEs: Peripheral neuropathy (80%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.18
4.5 mg 3 times / day multiple, oral Overdose Dose: 4.5 mg, 3 times / day Route: oral Route: multiple Dose: 4.5 mg, 3 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.18	unhealthy Health Status: unhealthy Condition: HIV infection Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.18	Other AEs: Peripheral neuropathy... Other AEs: Peripheral neuropathy (100%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.18
0.25 mg/kg 3 times / day multiple, oral Overdose Dose: 0.25 mg/kg, 3 times / day Route: oral Route: multiple Dose: 0.25 mg/kg, 3 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.18	unhealthy Health Status: unhealthy Condition: HIV infection Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.18	Disc. AE: Rash, Fever... AEs leading to discontinuation/dose reduction: Rash Fever Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.18
0.75 mg 3 times / day multiple, oral Recommended Dose: 0.75 mg, 3 times / day Route: oral Route: multiple Dose: 0.75 mg, 3 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.1	unhealthy Health Status: unhealthy Condition: HIV infection Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.1	Other AEs: Peripheral neuropathy... Other AEs: Peripheral neuropathy (grade 3-5) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.1
0.75 mg 3 times / day multiple, oral Recommended Dose: 0.75 mg, 3 times / day Route: oral Route: multiple Dose: 0.75 mg, 3 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.1, p.7	unhealthy Health Status: unhealthy Condition: HIV infection Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.1, p.7	Other AEs: Lactic acidosis, Hepatic steatosis... Other AEs: Lactic acidosis (grade 3-5) Hepatic steatosis (grade 3-5) Hepatic failure (grade 3-5) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.1, p.7
0.75 mg 3 times / day multiple, oral Recommended Dose: 0.75 mg, 3 times / day Route: oral Route: multiple Dose: 0.75 mg, 3 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.7	unhealthy Health Status: unhealthy Condition: HIV infection Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.7	Other AEs: Pancreatitis, Oral ulceration... Other AEs: Pancreatitis (grade 3-5, 1.1%) Oral ulceration (grade 3, 3%) Esophageal ulcer (grade 3) Cardiomyopathy (grade 3, infrequent) Congestive heart failure (grade 3, infrequent) Anaphylactoid reaction (grade 3) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s014lbl.pdf Page: p.7

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
	OAT1 294

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
OAT1 294	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/16724555/	not determined

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:10101	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:10101
ChemicalBook	CB2369466	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB2369466
MolPort	MolPort-002-885-873	https://www.molport.com/shop/molecule-link/MolPort-002-885-873
Selleck Chemicals	Zalcitabine	http://www.selleckchem.com/products/Zalcitabine.html
ZINC	ZINC000000039906	http://zinc15.docking.org/substances/ZINC000000039906
eMolecules	29549673	https://www.emolecules.com/cgi-bin/more?vid=29549673
eMolecules	501711	https://www.emolecules.com/cgi-bin/more?vid=501711

PubMed

Title	Date	PubMed
Effect of nucleoside analogs and non-nucleoside inhibitors of HIV-1 reverse transcriptase on cell-free virions.	1999	10226617
Synthesis and antiviral activity of 1-[1,5-dialkyl-1H-1,2,4-triazol-3-yl)methyl]thymines.	1999 Apr	10327888
ddC- and 3TC-bis(SATE) monophosphate prodrugs overcome cellular resistance mechanisms to HIV-1 associated with cytidine kinase deficiency.	1999 Apr-May	10432710
"Mixed inhibitors" of HIV-reverse transcriptase: synthesis and antiviral activity.	1999 Apr-May	10432669
Molecular mechanism of the short-term cardiotoxicity caused by 2',3'-dideoxycytidine (ddC): modulation of reactive oxygen species levels and ADP-ribosylation reactions.	1999 Dec 15	10591146
Relation of peripheral neuropathy to HIV treatment in four randomized clinical trials including didanosine.	1999 Jul	10463516
Mechanism of action and in vitro activity of 1',3'-dioxolanylpurine nucleoside analogues against sensitive and drug-resistant human immunodeficiency virus type 1 variants.	1999 Oct	10508010
Inhibitory effect of human immunodeficiency virus protease inhibitors on multidrug resistance transporter P-glycoproteins.	2000 Dec	11145192
In vitro selection of mutations in the human immunodeficiency virus type 1 reverse transcriptase that decrease susceptibility to (-)-beta-D-dioxolane-guanosine and suppress resistance to 3'-azido-3'-deoxythymidine.	2000 Jul	10858331
The molecular basis of inhibition and toxicity of modified cytosine analogues targetting HIV-1 reverse transcriptase.	2001	11594679
Peripheral neuropathy during stavudine-didanosine antiretroviral therapy.	2001 Apr	11737385
Determination of serum levels of thirteen human immunodeficiency virus-suppressing drugs by high-performance liquid chromatography.	2001 Apr 13	11355843
Synthesis and antiviral evaluation of C-4-hydrazide derivatives of 2',3'-dideoxycytidine.	2001 Apr-Jul	11562952
[Therapeutic aspects of HIV/AIDS infected patients and evaluation of therapeutic protocols].	2001 Dec	12113183
Antiviral activity of NMSO3 against adenovirus in vitro.	2001 Dec	11675145
Synthesis and chain length-anti-HIV activity relationship of fully N- and O-sulfated homooligomers of tyrosine.	2001 Feb	11249140
Antiretroviral treatments used among adults with HIV infection in Europe.	2001 Feb	11177461
MIKADO: a multicentre, open-label pilot study to evaluate the antiretroviral activity and safety of saquinavir with stavudine and zalcitabine.	2001 Jan	11737372
Phosphorylation of nucleoside analog antiretrovirals: a review for clinicians.	2001 Jan	11191730
Potential use of antiviral L(-)nucleoside analogues for the prevention or treatment of viral associated cancers.	2001 Jan	11164188
In vitro biological activity of prenylflavanones.	2001 Jan-Feb	11299746
Biological activity of kiwifruit peel extracts.	2001 Jun	11406859
Crystal structures of a ddATP-, ddTTP-, ddCTP, and ddGTP- trapped ternary complex of Klentaq1: insights into nucleotide incorporation and selectivity.	2001 Jun	11369861
Analysis of human immunodeficiency virus type 1 drug resistance in children receiving nucleoside analogue reverse-transcriptase inhibitors plus nevirapine, nelfinavir, or ritonavir (Pediatric AIDS Clinical Trials Group 377).	2001 Jun 15	11372025
Human cytosolic 5'-nucleotidase I: characterization and role in nucleoside analog resistance.	2001 Mar 30	11133996
Therapeutic effects of nucleoside analogues on psychomotor slowing in HIV infection.	2001 Mar 9	11242146
Differential human immunodeficiency virus-suppressive activity of reverse transcription inhibitors in resting and activated peripheral blood lymphocytes: implications for therapy.	2001 May-Jun	11572234
Mitochondrial alterations with mitochondrial DNA depletion in the nerves of AIDS patients with peripheral neuropathy induced by 2'3'-dideoxycytidine (ddC).	2001 Nov	11706061
Antitumor activity of 2',3'-dideoxycytidine nucleotide analog against tumors up-regulating DNA polymerase beta.	2001 Sep	11502887
"Senseless" antiviral polyribonucleotides: poly (1-propargylinosinic acid).	2002	11995639
The dangers of inferring treatment effects from observational data: a case study in HIV infection.	2002 Apr	11943438
Enhanced inhibition of orthopoxvirus replication in vitro by alkoxyalkyl esters of cidofovir and cyclic cidofovir.	2002 Apr	11897580
Broad nucleoside-analogue resistance implications for human immunodeficiency virus type 1 reverse-transcriptase mutations at codons 44 and 118.	2002 Apr 1	11920313
The distribution of the anti-HIV drug, 2'3'-dideoxycytidine (ddC), across the blood-brain and blood-cerebrospinal fluid barriers and the influence of organic anion transport inhibitors.	2002 Feb	11905988
S-acyl-2-thioethyl (SATE) pronucleotides are potent inhibitors of HIV-1 replication in T-lymphoid cells cross-resistant to deoxycytidine and thymidine analogs.	2002 Feb	11750940
Viral and immunologic follow up of 4 to 9 years of AIDS treatments by quadruple combinations of virostatics including integrase inhibitors applied in short sequences differing by drug rotation.	2002 Jan	11860730
ATP-dependent removal of nucleoside reverse transcriptase inhibitors by human immunodeficiency virus type 1 reverse transcriptase.	2002 Jul	12069972

Patents

Sample Use Guides

In Vivo Use Guide

Patients should be advised that HIVID is recommended for use in combination with active antiretroviral therapy. Greater activity has been observed when new antiretroviral therapies are begun at the same time as HIVID. Concomitant therapy should be based on a patient’s prior drug exposure. The recommended regimen is one 0.750 mg tablet of HIVID orally every 8 hours (2.25 mg HIVID total daily dose) in combination with other antiretroviral agents. Please refer to the complete product information for each of the other antiretroviral agents for the recommended doses of these agents. Based on preliminary data, the recommended HIVID dosage reduction for patients with impaired renal function is: creatinine clearance 10 to 40 mL/min: 0.750 mg of HIVID every 12 hours; creatinine clearance <10 mL/min: 0.750 mg of HIVID every 24 hours.

Route of Administration: Oral

In Vitro Use Guide

2',3'-Dideoxycytidine (DDC) was evaluated for prophylactic antiviral activity in vitro using the feline leukemia virus (FeLV)-cat animal model. In vitro antiviral activity of DDC against FeLV was dependent upon the target cell used for infection. DDC (5 to 10 microM) inhibited FeLV infection of feline lymphoid cells by greater than 80%, while 6.07 to 12.13 uM DDC was required to similarly inhibit infection of feline fibroblasts. However, 43 to 384 uM DDC was needed to inhibit FeLV infection of primary bone marrow cells by greater than 80%. These in vitro results suggest that, although relatively low doses of DDC may be adequate to prevent infection of feline lymphoid cells, 8- to 80-times-higher doses may be necessary to block infection of bone marrow cells, a primary target cell type for FeLV infection. Results of in vitro studies suggest that feline bone marrow cells may remain partially susceptible to FeLV infection at tolerated doses, while other somatic target tissues (i.e., lymphoid or epithelial tissues) may be protected from infection.

Name

Type

Language

ZALCITABINE

Official Name

English

ZALCITABINE [USAN]

Common Name

English

ZALCITABINE [ORANGE BOOK]

Common Name

English

2',3'-DIDEOXYCYTIDINE

Systematic Name

English

ZALCITABINE [WHO-DD]

Common Name

English

RO 24-2027/000

Code

English

ZALCITABINE [HSDB]

Common Name

English

ZALCITABINE [JAN]

Common Name

English

ZALCITABINE (DIDEOXYCYTIDINE,DDC) [VANDF]

Common Name

English

RO-24-2027/000

Code

English

HIVID

Brand Name

English

NSC-606170

Code

English

ZALCITABINE [IARC]

Common Name

English

ZALCITABINE [USP]

Common Name

English

ZALCITABINE [USP-RS]

Common Name

English

DIDEOXYCYTIDINE

Systematic Name

English

RO-242027000

Code

English

ZALCITABINE [MART.]

Common Name

English

ZALCITABINE [VANDF]

Common Name

English

DDC

Common Name

English

CYTIDINE, 2',3'-DIDEOXY-

Systematic Name

English

ZALCITABINE [INN]

Common Name

English

ZALCITABINE [MI]

Common Name

English

RO-24-2027000

Code

English

Classification Tree Code System Code

WHO-VATC

QJ05AF03