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
Molecular Formula | C9H13N3O3 |
Molecular Weight | 211.2178 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
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 |
---|---|---|
ddC- and 3TC-bis(SATE) monophosphate prodrugs overcome cellular resistance mechanisms to HIV-1 associated with cytidine kinase deficiency. | 1999 Apr-May |
|
Activities of masked 2',3'-dideoxynucleoside monophosphate derivatives against human immunodeficiency virus in resting macrophages. | 2000 Jan |
|
Potentiation of the anti-HIV activity of zalcitabine and lamivudine by a CTP synthase inhibitor, 3-deazauridine. | 2000 Jan-Feb |
|
Selection and characterization of human immunodeficiency virus type 1 variants resistant to the (+) and (-) enantiomers of 2'-deoxy-3'-oxa-4'-thio-5-fluorocytidine. | 2000 May |
|
Determination of serum levels of thirteen human immunodeficiency virus-suppressing drugs by high-performance liquid chromatography. | 2001 Apr 13 |
|
Susceptibility of human T cell leukemia virus type 1 to reverse-transcriptase inhibitors: evidence for resistance to lamivudine. | 2001 Aug 15 |
|
Simultaneous quantitation of nucleoside HIV-1 reverse transcriptase inhibitors by short-end injection capillary electrochromatography on a beta-cyclodextrin-bonded silica stationary phase. | 2001 Aug 24 |
|
Synthesis and chain length-anti-HIV activity relationship of fully N- and O-sulfated homooligomers of tyrosine. | 2001 Feb |
|
MIKADO: a multicentre, open-label pilot study to evaluate the antiretroviral activity and safety of saquinavir with stavudine and zalcitabine. | 2001 Jan |
|
Phosphorylation of nucleoside analog antiretrovirals: a review for clinicians. | 2001 Jan |
|
Crystal structures of a ddATP-, ddTTP-, ddCTP, and ddGTP- trapped ternary complex of Klentaq1: insights into nucleotide incorporation and selectivity. | 2001 Jun |
|
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 |
|
Differential incorporation and removal of antiviral deoxynucleotides by human DNA polymerase gamma. | 2001 Jun 29 |
|
Functional characterization of rat organic anion transporter 2 in LLC-PK1 cells. | 2001 Sep |
|
Mismatched double-stranded RNA (polyI-polyC(12)U) is synergistic with multiple anti-HIV drugs and is active against drug-sensitive and drug-resistant HIV-1 in vitro. | 2001 Sep |
|
Novel direct detection method for quantitative determination of intracellular nucleoside triphosphates using weak anion exchange liquid chromatography/tandem mass spectrometry. | 2002 |
|
New developments in anti-HIV chemotherapy. | 2002 Jul 18 |
|
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 |
|
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 |
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.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 05:31:55 UTC 2023
by
admin
on
Sat Dec 16 05:31:55 UTC 2023
|
Record UNII |
6L3XT8CB3I
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
WHO-VATC |
QJ05AF03
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
||
|
WHO-ATC |
J05AF03
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
||
|
FDA ORPHAN DRUG |
17586
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
||
|
FDA ORPHAN DRUG |
28388
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
||
|
NCI_THESAURUS |
C1557
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
||
|
LIVERTOX |
1044
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
DTXSID0023747
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | |||
|
CC-48
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | |||
|
1724306
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | |||
|
ZALCITABINE
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | |||
|
24066
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | |||
|
606170
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | |||
|
CHEMBL853
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | |||
|
m11577
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | Merck Index | ||
|
6L3XT8CB3I
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | |||
|
3363
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | RxNorm | ||
|
C430
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | |||
|
6871
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | |||
|
DB00943
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | |||
|
D016047
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | |||
|
10101
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | |||
|
100000079386
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | |||
|
2856
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | |||
|
4828
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | |||
|
7481-89-2
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY | |||
|
SUB00130MIG
Created by
admin on Sat Dec 16 05:31:55 UTC 2023 , Edited by admin on Sat Dec 16 05:31:55 UTC 2023
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |