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
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
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 |
---|---|---|
Effect of nucleoside analogs and non-nucleoside inhibitors of HIV-1 reverse transcriptase on cell-free virions. | 1999 |
|
Synthesis and antiviral activity of 1-[1,5-dialkyl-1H-1,2,4-triazol-3-yl)methyl]thymines. | 1999 Apr |
|
ddC- and 3TC-bis(SATE) monophosphate prodrugs overcome cellular resistance mechanisms to HIV-1 associated with cytidine kinase deficiency. | 1999 Apr-May |
|
"Mixed inhibitors" of HIV-reverse transcriptase: synthesis and antiviral activity. | 1999 Apr-May |
|
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 |
|
Relation of peripheral neuropathy to HIV treatment in four randomized clinical trials including didanosine. | 1999 Jul |
|
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 |
|
Inhibitory effect of human immunodeficiency virus protease inhibitors on multidrug resistance transporter P-glycoproteins. | 2000 Dec |
|
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 |
|
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 |
|
Determination of serum levels of thirteen human immunodeficiency virus-suppressing drugs by high-performance liquid chromatography. | 2001 Apr 13 |
|
Synthesis and antiviral evaluation of C-4-hydrazide derivatives of 2',3'-dideoxycytidine. | 2001 Apr-Jul |
|
[Therapeutic aspects of HIV/AIDS infected patients and evaluation of therapeutic protocols]. | 2001 Dec |
|
Antiviral activity of NMSO3 against adenovirus in vitro. | 2001 Dec |
|
Synthesis and chain length-anti-HIV activity relationship of fully N- and O-sulfated homooligomers of tyrosine. | 2001 Feb |
|
Antiretroviral treatments used among adults with HIV infection in Europe. | 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 |
|
Potential use of antiviral L(-)nucleoside analogues for the prevention or treatment of viral associated cancers. | 2001 Jan |
|
In vitro biological activity of prenylflavanones. | 2001 Jan-Feb |
|
Biological activity of kiwifruit peel extracts. | 2001 Jun |
|
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 |
|
Human cytosolic 5'-nucleotidase I: characterization and role in nucleoside analog resistance. | 2001 Mar 30 |
|
Therapeutic effects of nucleoside analogues on psychomotor slowing in HIV infection. | 2001 Mar 9 |
|
Differential human immunodeficiency virus-suppressive activity of reverse transcription inhibitors in resting and activated peripheral blood lymphocytes: implications for therapy. | 2001 May-Jun |
|
Mitochondrial alterations with mitochondrial DNA depletion in the nerves of AIDS patients with peripheral neuropathy induced by 2'3'-dideoxycytidine (ddC). | 2001 Nov |
|
Antitumor activity of 2',3'-dideoxycytidine nucleotide analog against tumors up-regulating DNA polymerase beta. | 2001 Sep |
|
"Senseless" antiviral polyribonucleotides: poly (1-propargylinosinic acid). | 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 |
|
Broad nucleoside-analogue resistance implications for human immunodeficiency virus type 1 reverse-transcriptase mutations at codons 44 and 118. | 2002 Apr 1 |
|
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 |
|
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 |
|
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 |
|
ATP-dependent removal of nucleoside reverse transcriptase inhibitors by human immunodeficiency virus type 1 reverse transcriptase. | 2002 Jul |
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 Jun 26 00:39:30 UTC 2021 , Edited by admin on Sat Jun 26 00:39:30 UTC 2021
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WHO-ATC |
J05AF03
Created by
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FDA ORPHAN DRUG |
17586
Created by
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FDA ORPHAN DRUG |
28388
Created by
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NCI_THESAURUS |
C1557
Created by
admin on Sat Jun 26 00:39:30 UTC 2021 , Edited by admin on Sat Jun 26 00:39:30 UTC 2021
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LIVERTOX |
1044
Created by
admin on Sat Jun 26 00:39:30 UTC 2021 , Edited by admin on Sat Jun 26 00:39:30 UTC 2021
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Code System | Code | Type | Description | ||
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7481-89-2
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ZALCITABINE
Created by
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1724306
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24066
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PRIMARY | |||
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CHEMBL853
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M11577
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6L3XT8CB3I
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3363
Created by
admin on Sat Jun 26 00:39:30 UTC 2021 , Edited by admin on Sat Jun 26 00:39:30 UTC 2021
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C430
Created by
admin on Sat Jun 26 00:39:30 UTC 2021 , Edited by admin on Sat Jun 26 00:39:30 UTC 2021
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6871
Created by
admin on Sat Jun 26 00:39:30 UTC 2021 , Edited by admin on Sat Jun 26 00:39:30 UTC 2021
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DB00943
Created by
admin on Sat Jun 26 00:39:30 UTC 2021 , Edited by admin on Sat Jun 26 00:39:30 UTC 2021
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D016047
Created by
admin on Sat Jun 26 00:39:30 UTC 2021 , Edited by admin on Sat Jun 26 00:39:30 UTC 2021
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2856
Created by
admin on Sat Jun 26 00:39:30 UTC 2021 , Edited by admin on Sat Jun 26 00:39:30 UTC 2021
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4828
Created by
admin on Sat Jun 26 00:39:30 UTC 2021 , Edited by admin on Sat Jun 26 00:39:30 UTC 2021
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7481-89-2
Created by
admin on Sat Jun 26 00:39:30 UTC 2021 , Edited by admin on Sat Jun 26 00:39:30 UTC 2021
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SUB00130MIG
Created by
admin on Sat Jun 26 00:39:30 UTC 2021 , Edited by admin on Sat Jun 26 00:39:30 UTC 2021
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ACTIVE MOIETY