Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C9H13N3O3 |
Molecular Weight | 211.2178 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=NC(=O)N(C=C1)[C@H]2CC[C@@H](CO)O2
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
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9736530
Curator's Comment: Known to be CNS penetrant in rat. Human data not available
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL247 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9179531 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | HIVID Approved UseHIVID 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 Date7.0891202E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
7.6 μg/L |
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 |
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 |
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 |
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 |
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 |
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 | Co-administered | Analyte | Population |
---|---|---|---|---|
0.018 mg × h/L |
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 |
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 |
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 |
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 |
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 |
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 |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.5 h |
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 |
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 |
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 |
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 |
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 |
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 |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
96% |
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% |
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: Page: p.858 |
unhealthy, 26-57 n = 5 Health Status: unhealthy Condition: HIV infection Age Group: 26-57 Sex: M Population Size: 5 Sources: Page: p.858 |
Disc. AE: Peripheral neuropathy, Leukopenia... AEs leading to discontinuation/dose reduction: Peripheral neuropathy (40%) Sources: Page: p.858Leukopenia (20%) Thrombocytopenia (40%) |
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: Page: p.191 |
unhealthy, 42 n = 18 Health Status: unhealthy Condition: HIV infection Age Group: 42 Sex: M+F Population Size: 18 Sources: Page: p.191 |
Disc. AE: Peripheral neuropathy... AEs leading to discontinuation/dose reduction: Peripheral neuropathy (grade 3, 100%) Sources: 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: Page: p.191 |
unhealthy, 42 n = 18 Health Status: unhealthy Condition: HIV infection Age Group: 42 Sex: M+F Population Size: 18 Sources: Page: p.191 |
Disc. AE: Peripheral neuropathy... AEs leading to discontinuation/dose reduction: Peripheral neuropathy (grade 3, 100%) Sources: 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: Page: p.18 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.18 |
Other AEs: Peripheral neuropathy... Other AEs: Peripheral neuropathy (80%) Sources: 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: Page: p.18 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.18 |
Other AEs: Peripheral neuropathy... Other AEs: Peripheral neuropathy (100%) Sources: 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: Page: p.18 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.18 |
Disc. AE: Rash, Fever... AEs leading to discontinuation/dose reduction: Rash Sources: Page: p.18Fever |
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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.1 |
Other AEs: Peripheral neuropathy... Other AEs: Peripheral neuropathy (grade 3-5) Sources: 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: Page: p.1, p.7 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.1, p.7 |
Other AEs: Lactic acidosis, Hepatic steatosis... Other AEs: Lactic acidosis (grade 3-5) Sources: Page: p.1, p.7Hepatic steatosis (grade 3-5) Hepatic failure (grade 3-5) |
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: Page: p.7 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.7 |
Other AEs: Pancreatitis, Oral ulceration... Other AEs: Pancreatitis (grade 3-5, 1.1%) Sources: Page: p.7Oral ulceration (grade 3, 3%) Esophageal ulcer (grade 3) Cardiomyopathy (grade 3, infrequent) Congestive heart failure (grade 3, infrequent) Anaphylactoid reaction (grade 3) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Leukopenia | 20% Disc. AE |
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: Page: p.858 |
unhealthy, 26-57 n = 5 Health Status: unhealthy Condition: HIV infection Age Group: 26-57 Sex: M Population Size: 5 Sources: Page: p.858 |
Peripheral neuropathy | 40% Disc. AE |
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: Page: p.858 |
unhealthy, 26-57 n = 5 Health Status: unhealthy Condition: HIV infection Age Group: 26-57 Sex: M Population Size: 5 Sources: Page: p.858 |
Thrombocytopenia | 40% Disc. AE |
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: Page: p.858 |
unhealthy, 26-57 n = 5 Health Status: unhealthy Condition: HIV infection Age Group: 26-57 Sex: M Population Size: 5 Sources: Page: p.858 |
Peripheral neuropathy | grade 3, 100% Disc. AE |
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: Page: p.191 |
unhealthy, 42 n = 18 Health Status: unhealthy Condition: HIV infection Age Group: 42 Sex: M+F Population Size: 18 Sources: Page: p.191 |
Peripheral neuropathy | grade 3, 100% Disc. AE |
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: Page: p.191 |
unhealthy, 42 n = 18 Health Status: unhealthy Condition: HIV infection Age Group: 42 Sex: M+F Population Size: 18 Sources: Page: p.191 |
Peripheral neuropathy | 80% | 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: Page: p.18 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.18 |
Peripheral neuropathy | 100% | 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: Page: p.18 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.18 |
Fever | Disc. AE | 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: Page: p.18 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.18 |
Rash | Disc. AE | 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: Page: p.18 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.18 |
Peripheral neuropathy | grade 3-5 | 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: Page: p.1 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.1 |
Hepatic failure | grade 3-5 | 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: Page: p.1, p.7 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.1, p.7 |
Hepatic steatosis | grade 3-5 | 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: Page: p.1, p.7 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.1, p.7 |
Lactic acidosis | grade 3-5 | 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: Page: p.1, p.7 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.1, p.7 |
Anaphylactoid reaction | grade 3 | 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: Page: p.7 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.7 |
Esophageal ulcer | grade 3 | 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: Page: p.7 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.7 |
Oral ulceration | grade 3, 3% | 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: Page: p.7 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.7 |
Cardiomyopathy | grade 3, infrequent | 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: Page: p.7 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.7 |
Congestive heart failure | grade 3, infrequent | 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: Page: p.7 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.7 |
Pancreatitis | grade 3-5, 1.1% | 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: Page: p.7 |
unhealthy Health Status: unhealthy Condition: HIV infection Sources: Page: p.7 |
PubMed
Title | Date | PubMed |
---|---|---|
Human immunodeficiency virus 1 strains resistant to nucleoside inhibitors of reverse transcriptase in isolates from the Czech Republic as monitored by line probe assay and nucleotide sequencing. | 2001 |
|
Mutational patterns in the HIV genome and cross-resistance following nucleoside and nucleotide analogue drug exposure. | 2001 |
|
DABOs as candidates to prevent mucosal HIV transmission. | 2001 |
|
The molecular basis of inhibition and toxicity of modified cytosine analogues targetting HIV-1 reverse transcriptase. | 2001 |
|
Peripheral neuropathy during stavudine-didanosine antiretroviral therapy. | 2001 Apr |
|
Synthesis and antiviral evaluation of C-4-hydrazide derivatives of 2',3'-dideoxycytidine. | 2001 Apr-Jul |
|
Testing the reverse transcriptase model of somatic mutation. | 2001 Aug |
|
Do HIV type 1 RNA levels provide additional prognostic value to CD4(+) T lymphocyte counts in patients with advanced HIV type 1 infection? | 2001 Aug 10 |
|
Susceptibility of human T cell leukemia virus type 1 to reverse-transcriptase inhibitors: evidence for resistance to lamivudine. | 2001 Aug 15 |
|
[Therapeutic aspects of HIV/AIDS infected patients and evaluation of therapeutic protocols]. | 2001 Dec |
|
HIV-1 reverse transcriptase mutations found in a drug-experienced patient confer reduced susceptibility to multiple nucleoside reverse transcriptase inhibitors. | 2001 Dec |
|
Antiviral activity of NMSO3 against adenovirus in vitro. | 2001 Dec |
|
MIKADO: a multicentre, open-label pilot study to evaluate the antiretroviral activity and safety of saquinavir with stavudine and zalcitabine. | 2001 Jan |
|
Eruptive cheilitis: a new adverse effect in reactive HIV-positive patients subjected to high activity antiretroviral therapy (HAART). Presentation of six clinical cases. | 2001 Jan-Feb |
|
Differential susceptibility of retroviruses to nucleoside analogues. | 2001 Mar |
|
Mitochondrial alterations with mitochondrial DNA depletion in the nerves of AIDS patients with peripheral neuropathy induced by 2'3'-dideoxycytidine (ddC). | 2001 Nov |
|
New developments in anti-HIV chemotherapy. | 2001 Nov |
|
Anti-human immunodeficiency virus drugs are ineffective against Pneumocystis carinii in vitro and in vivo. | 2001 Nov 15 |
|
HIV-protease inhibitors alter retinoic acid synthesis. | 2001 Oct 19 |
|
Functional characterization of rat organic anion transporter 2 in LLC-PK1 cells. | 2001 Sep |
|
Antitumor activity of 2',3'-dideoxycytidine nucleotide analog against tumors up-regulating DNA polymerase beta. | 2001 Sep |
|
A preliminary benefit-risk assessment of lamivudine for the treatment of chronic hepatitis B virus infection. | 2002 |
|
"Senseless" antiviral polyribonucleotides: poly (1-propargylinosinic acid). | 2002 |
|
Novel direct detection method for quantitative determination of intracellular nucleoside triphosphates using weak anion exchange liquid chromatography/tandem mass spectrometry. | 2002 |
|
Fomivirsen: clinical pharmacology and potential drug interactions. | 2002 |
|
The dangers of inferring treatment effects from observational data: a case study in HIV infection. | 2002 Apr |
|
Enhanced inhibition of orthopoxvirus replication in vitro by alkoxyalkyl esters of cidofovir and cyclic cidofovir. | 2002 Apr |
|
Tenofovir exhibits low cytotoxicity in various human cell types: comparison with other nucleoside reverse transcriptase inhibitors. | 2002 Apr |
|
Broad nucleoside-analogue resistance implications for human immunodeficiency virus type 1 reverse-transcriptase mutations at codons 44 and 118. | 2002 Apr 1 |
|
Molecular basis of 2',3'-dideoxycytidine-induced drug resistance in human cells. | 2002 Feb |
|
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 |
|
Involvement of DNA polymerase beta in DNA replication and mutagenic consequences. | 2002 Feb 1 |
|
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 |
|
Uptake of lamivudine by rat renal brush border membrane vesicles. | 2002 Jan |
|
Transbuccal delivery of 2',3'-dideoxycytidine: in vitro permeation study and histological investigation. | 2002 Jan 1 |
|
ATP-dependent removal of nucleoside reverse transcriptase inhibitors by human immunodeficiency virus type 1 reverse transcriptase. | 2002 Jul |
|
An ancient prevertebrate Na+-nucleoside cotransporter (hfCNT) from the Pacific hagfish (Eptatretus stouti). | 2002 Jul |
|
3'-Azido-2',3'-dideoxythymidine induced deficiency of thymidine kinases 1, 2 and deoxycytidine kinase in H9 T-lymphoid cells. | 2002 Jul 15 |
|
Perspectives on the molecular mechanism of inhibition and toxicity of nucleoside analogs that target HIV-1 reverse transcriptase. | 2002 Jul 18 |
|
New developments in anti-HIV chemotherapy. | 2002 Jul 18 |
|
Prevalence of HIV-1 polymerase gene mutations in pre-treated patients in Thailand. | 2002 Mar |
|
Observations of HIV-1 genotypic drug resistance in a trial of four reverse transcriptase inhibitors (Quattro Trial). | 2002 Mar |
|
ViroLogic announces agreement with Achillion. | 2002 Mar |
|
Novel use of a guanosine prodrug approach to convert 2',3'-didehydro-2',3'-dideoxyguanosine into a viable antiviral agent. | 2002 Mar |
|
Assessment of mitochondrial toxicity in human cells treated with tenofovir: comparison with other nucleoside reverse transcriptase inhibitors. | 2002 Mar |
|
Dietary supplements in the treatment of nucleoside reverse transcriptase inhibitor-related mitochondrial toxicity. | 2002 Mar 29 |
|
Concurrent analysis of nucleoside reverse transcriptase inhibitors in a pool of endogenous nucleosides by short-end injection-capillary electrochromatography on a beta-cyclodextrin-bonded stationary phase. | 2002 May |
|
Certification of the critical importance of L-3-(2-naphthyl)alanine at position 3 of a specific CXCR4 inhibitor, T140, leads to an exploratory performance of its downsizing study. | 2002 May |
|
Impact of highly active antiretroviral therapy on cognitive processing in HIV infection: cross-sectional and longitudinal studies of event-related potentials. | 2002 May 1 |
|
Point mutations and deletions in the znfn1a1/ikaros gene in chemically induced murine lymphomas. | 2002 May 1 |
Sample Use Guides
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2167039
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.
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Classification Tree | Code System | Code | ||
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WHO-VATC |
QJ05AF03
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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WHO-ATC |
J05AF03
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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FDA ORPHAN DRUG |
17586
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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FDA ORPHAN DRUG |
28388
Created by
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NCI_THESAURUS |
C1557
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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LIVERTOX |
1044
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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DTXSID0023747
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PRIMARY | |||
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CC-48
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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1724306
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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ZALCITABINE
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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24066
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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6L3XT8CB3I
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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606170
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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CHEMBL853
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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M11577
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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PRIMARY | Merck Index | ||
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6L3XT8CB3I
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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3363
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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PRIMARY | RxNorm | ||
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C430
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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6871
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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DB00943
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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D016047
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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10101
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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2856
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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4828
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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7481-89-2
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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SUB00130MIG
Created by
admin on Sat Dec 17 18:29:10 UTC 2022 , Edited by admin on Sat Dec 17 18:29:10 UTC 2022
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ACTIVE MOIETY