Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C10H12N4O3 |
| Molecular Weight | 236.2273 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC[C@@H]1CC[C@@H](O1)N2C=NC3=C2N=CNC3=O
InChI
InChIKey=BXZVVICBKDXVGW-NKWVEPMBSA-N
InChI=1S/C10H12N4O3/c15-3-6-1-2-7(17-6)14-5-13-8-9(14)11-4-12-10(8)16/h4-7,15H,1-3H2,(H,11,12,16)/t6-,7+/m0/s1
| Molecular Formula | C10H12N4O3 |
| Molecular Weight | 236.2273 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: description was created based on several sources, including https://www.ott.nih.gov/sites/default/files/documents/pdfs/VidexCS.pdf
Curator's Comment: description was created based on several sources, including https://www.ott.nih.gov/sites/default/files/documents/pdfs/VidexCS.pdf
Didanosine was developed by Bristol-Myers Squibb in collaboration with the NIH for the treatment of HIV-1 infections. Upon administration the drug is metabolized to the active metabolite which inhibits HIV-1 reverse transcriptase both by competing with deoxyadenosine 5'-triphosphate and by its incorporation into viral DNA. Didanosine was approved by FDA under the name Videx (among the other names).
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22514580
Curator's Comment: In animal models, didanosine was able to cross the BBB using saturable and non–saturable mechanisms.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL247 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | VIDEX Approved UseVidex (didanosine, USP) is a nucleoside reverse transcriptase inhibitor for use in combination with other antiretroviral agents for the treatment of human immunodeficiency virus (HIV)-1 infection. Launch Date1991 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
305 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
0.4 mg/kg bw single, intravenous dose: 0.4 mg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
291 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
0.4 mg/kg bw 2 times / day steady-state, intravenous dose: 0.4 mg/kg bw route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2818 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
3 mg/kg bw single, intravenous dose: 3 mg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3041 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
3 mg/kg bw 2 times / day steady-state, intravenous dose: 3 mg/kg bw route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
17974 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
16.5 mg/kg bw single, intravenous dose: 16.5 mg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
18019 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
16.5 mg/kg bw 2 times / day steady-state, intravenous dose: 16.5 mg/kg bw route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
244 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
0.8 mg/kg bw single, oral dose: 0.8 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
343 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
0.8 mg/kg bw 2 times / day steady-state, oral dose: 0.8 mg/kg bw route of administration: Oral experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1494 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
6 mg/kg bw single, oral dose: 6 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2257 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
6 mg/kg bw 2 times / day steady-state, oral dose: 6 mg/kg bw route of administration: Oral experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
5787 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
33 mg/kg bw single, oral dose: 33 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
6041 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
33 mg/kg bw 2 times / day steady-state, oral dose: 33 mg/kg bw route of administration: Oral experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
413 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
0.4 mg/kg bw single, intravenous dose: 0.4 mg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
418 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
0.4 mg/kg bw 2 times / day steady-state, intravenous dose: 0.4 mg/kg bw route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3726 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
3 mg/kg bw single, intravenous dose: 3 mg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
4118 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
3 mg/kg bw 2 times / day steady-state, intravenous dose: 3 mg/kg bw route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
28257 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
16.5 mg/kg bw single, intravenous dose: 16.5 mg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
32264 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
16.5 mg/kg bw 2 times / day steady-state, intravenous dose: 16.5 mg/kg bw route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
351 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
0.8 mg/kg bw single, oral dose: 0.8 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
421 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
0.8 mg/kg bw 2 times / day steady-state, oral dose: 0.8 mg/kg bw route of administration: Oral experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2374 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
6 mg/kg bw single, oral dose: 6 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3377 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
6 mg/kg bw 2 times / day steady-state, oral dose: 6 mg/kg bw route of administration: Oral experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
12730 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
33 mg/kg bw single, oral dose: 33 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
14179 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
33 mg/kg bw 2 times / day steady-state, oral dose: 33 mg/kg bw route of administration: Oral experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.88 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
0.4 mg/kg bw single, intravenous dose: 0.4 mg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
0.93 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
0.4 mg/kg bw 2 times / day steady-state, intravenous dose: 0.4 mg/kg bw route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1.17 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
3 mg/kg bw single, intravenous dose: 3 mg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1.19 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
3 mg/kg bw 2 times / day steady-state, intravenous dose: 3 mg/kg bw route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1.48 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
16.5 mg/kg bw single, intravenous dose: 16.5 mg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1.49 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
16.5 mg/kg bw 2 times / day steady-state, intravenous dose: 16.5 mg/kg bw route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
0.76 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
0.8 mg/kg bw single, oral dose: 0.8 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
0.8 mg/kg bw 2 times / day steady-state, oral dose: 0.8 mg/kg bw route of administration: Oral experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1.12 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
6 mg/kg bw single, oral dose: 6 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1.24 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
6 mg/kg bw 2 times / day steady-state, oral dose: 6 mg/kg bw route of administration: Oral experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1.64 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
33 mg/kg bw single, oral dose: 33 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1903100/ |
33 mg/kg bw 2 times / day steady-state, oral dose: 33 mg/kg bw route of administration: Oral experiment type: STEADY-STATE co-administered: |
DIDANOSINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
25 mg/kg 1 times / day steady, oral Highest studied dose Dose: 25 mg/kg, 1 times / day Route: oral Route: steady Dose: 25 mg/kg, 1 times / day Sources: |
unhealthy, 0.7 - 18.9 years Health Status: unhealthy Age Group: 0.7 - 18.9 years Sex: M+F Sources: |
DLT: Neuropathy, Pancreatitis... Dose limiting toxicities: Neuropathy (13 patients) Sources: Pancreatitis (6 patients) |
12.8 mg/kg 1 times / day steady, oral Recommended Dose: 12.8 mg/kg, 1 times / day Route: oral Route: steady Dose: 12.8 mg/kg, 1 times / day Sources: |
unhealthy, 0.7 - 18.9 years Health Status: unhealthy Age Group: 0.7 - 18.9 years Sex: M+F Sources: |
DLT: Neuropathy, Pancreatitis... Dose limiting toxicities: Neuropathy (5 patients) Sources: Pancreatitis (1 patient) |
13 mg/kg 1 times / day steady, oral Recommended Dose: 13 mg/kg, 1 times / day Route: oral Route: steady Dose: 13 mg/kg, 1 times / day Sources: |
unhealthy, 0.7 - 18.9 years Health Status: unhealthy Age Group: 0.7 - 18.9 years Sex: M+F Sources: |
DLT: Pancreatitis... Dose limiting toxicities: Pancreatitis (grade 5, 0.35%) Sources: |
20.5 mg/kg 1 times / day steady, oral Recommended Dose: 20.5 mg/kg, 1 times / day Route: oral Route: steady Dose: 20.5 mg/kg, 1 times / day Sources: |
unhealthy, 0.7 - 18.9 years Health Status: unhealthy Age Group: 0.7 - 18.9 years Sex: M+F Sources: |
DLT: Neuropathy, Pancreatitis... Dose limiting toxicities: Neuropathy (8 patients) Sources: Pancreatitis (10 patients) |
500 mg 1 times / day steady, oral Recommended Dose: 500 mg, 1 times / day Route: oral Route: steady Dose: 500 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: |
DLT: Neutropenia, Neutropenia... Disc. AE: Anemia, Thrombocytopenia... Dose limiting toxicities: Neutropenia (grade 4, 3 patients) AEs leading toNeutropenia (grade 3, 9 patients) Neuropathy (5 patients) Diarrhea (3 patients) Pancreatitis (2 patients) Serum alkaline phosphatase elevated (2 patients) Abdominal pain (1 patient) discontinuation/dose reduction: Anemia (grade 3, 4 patients) Sources: Thrombocytopenia (grade 3, 1 patient) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Neuropathy | 13 patients DLT, Disc. AE |
25 mg/kg 1 times / day steady, oral Highest studied dose Dose: 25 mg/kg, 1 times / day Route: oral Route: steady Dose: 25 mg/kg, 1 times / day Sources: |
unhealthy, 0.7 - 18.9 years Health Status: unhealthy Age Group: 0.7 - 18.9 years Sex: M+F Sources: |
| Pancreatitis | 6 patients DLT, Disc. AE |
25 mg/kg 1 times / day steady, oral Highest studied dose Dose: 25 mg/kg, 1 times / day Route: oral Route: steady Dose: 25 mg/kg, 1 times / day Sources: |
unhealthy, 0.7 - 18.9 years Health Status: unhealthy Age Group: 0.7 - 18.9 years Sex: M+F Sources: |
| Pancreatitis | 1 patient DLT, Disc. AE |
12.8 mg/kg 1 times / day steady, oral Recommended Dose: 12.8 mg/kg, 1 times / day Route: oral Route: steady Dose: 12.8 mg/kg, 1 times / day Sources: |
unhealthy, 0.7 - 18.9 years Health Status: unhealthy Age Group: 0.7 - 18.9 years Sex: M+F Sources: |
| Neuropathy | 5 patients DLT, Disc. AE |
12.8 mg/kg 1 times / day steady, oral Recommended Dose: 12.8 mg/kg, 1 times / day Route: oral Route: steady Dose: 12.8 mg/kg, 1 times / day Sources: |
unhealthy, 0.7 - 18.9 years Health Status: unhealthy Age Group: 0.7 - 18.9 years Sex: M+F Sources: |
| Pancreatitis | grade 5, 0.35% DLT, Disc. AE |
13 mg/kg 1 times / day steady, oral Recommended Dose: 13 mg/kg, 1 times / day Route: oral Route: steady Dose: 13 mg/kg, 1 times / day Sources: |
unhealthy, 0.7 - 18.9 years Health Status: unhealthy Age Group: 0.7 - 18.9 years Sex: M+F Sources: |
| Pancreatitis | 10 patients DLT, Disc. AE |
20.5 mg/kg 1 times / day steady, oral Recommended Dose: 20.5 mg/kg, 1 times / day Route: oral Route: steady Dose: 20.5 mg/kg, 1 times / day Sources: |
unhealthy, 0.7 - 18.9 years Health Status: unhealthy Age Group: 0.7 - 18.9 years Sex: M+F Sources: |
| Neuropathy | 8 patients DLT, Disc. AE |
20.5 mg/kg 1 times / day steady, oral Recommended Dose: 20.5 mg/kg, 1 times / day Route: oral Route: steady Dose: 20.5 mg/kg, 1 times / day Sources: |
unhealthy, 0.7 - 18.9 years Health Status: unhealthy Age Group: 0.7 - 18.9 years Sex: M+F Sources: |
| Abdominal pain | 1 patient DLT, Disc. AE |
500 mg 1 times / day steady, oral Recommended Dose: 500 mg, 1 times / day Route: oral Route: steady Dose: 500 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: |
| Pancreatitis | 2 patients DLT, Disc. AE |
500 mg 1 times / day steady, oral Recommended Dose: 500 mg, 1 times / day Route: oral Route: steady Dose: 500 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: |
| Serum alkaline phosphatase elevated | 2 patients DLT, Disc. AE |
500 mg 1 times / day steady, oral Recommended Dose: 500 mg, 1 times / day Route: oral Route: steady Dose: 500 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: |
| Diarrhea | 3 patients DLT, Disc. AE |
500 mg 1 times / day steady, oral Recommended Dose: 500 mg, 1 times / day Route: oral Route: steady Dose: 500 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: |
| Neuropathy | 5 patients DLT, Disc. AE |
500 mg 1 times / day steady, oral Recommended Dose: 500 mg, 1 times / day Route: oral Route: steady Dose: 500 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: |
| Thrombocytopenia | grade 3, 1 patient Disc. AE |
500 mg 1 times / day steady, oral Recommended Dose: 500 mg, 1 times / day Route: oral Route: steady Dose: 500 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: |
| Anemia | grade 3, 4 patients Disc. AE |
500 mg 1 times / day steady, oral Recommended Dose: 500 mg, 1 times / day Route: oral Route: steady Dose: 500 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: |
| Neutropenia | grade 3, 9 patients DLT, Disc. AE |
500 mg 1 times / day steady, oral Recommended Dose: 500 mg, 1 times / day Route: oral Route: steady Dose: 500 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: |
| Neutropenia | grade 4, 3 patients DLT, Disc. AE |
500 mg 1 times / day steady, oral Recommended Dose: 500 mg, 1 times / day Route: oral Route: steady Dose: 500 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Comparison of genotypic and phenotypic resistance patterns of human immunodeficiency virus type 1 isolates from patients treated with stavudine and didanosine or zidovudine and lamivudine. | 2001-09-15 |
|
| Novel low molecular weight spirodiketopiperazine derivatives potently inhibit R5 HIV-1 infection through their antagonistic effects on CCR5. | 2001-09-14 |
|
| Immunological and virological effects of long term IL-2 therapy in HIV-1-infected patients. | 2001-09-07 |
|
| Direct analysis of mitochondrial toxicity of antiretroviral drugs. | 2001-09-07 |
|
| Novel deletion of HIV type 1 reverse transcriptase residue 69 conferring selective high-level resistance to nevirapine. | 2001-09-01 |
|
| Liver failure after long-term nucleoside antiretroviral therapy. | 2001-09-01 |
|
| 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. | 2001-09 |
|
| [Immunologic response to antiretroviral treatment with combined stavudine, didanosine and nevirapine]. | 2001-08-17 |
|
| Susceptibility of human T cell leukemia virus type 1 to reverse-transcriptase inhibitors: evidence for resistance to lamivudine. | 2001-08-15 |
|
| Eruptive cheilitis: a new adverse effect in reactive HIV-positive patients subjected to high activity antiretroviral therapy (HAART). Presentation of six clinical cases. | 2001-08-08 |
|
| Antiviral drugs: current state of the art. | 2001-08 |
|
| Effects of treatment intensification with hydroxyurea in HIV-infected patients with virologic suppression. | 2001-07-27 |
|
| Transport of antiviral 3'-deoxy-nucleoside drugs by recombinant human and rat equilibrative, nitrobenzylthioinosine (NBMPR)-insensitive (ENT2) nucleoside transporter proteins produced in Xenopus oocytes. | 2001-07-21 |
|
| Warning for pregnant women on HIV therapy. | 2001-07-19 |
|
| Development of drug resistance in patients receiving combinations of zidovudine, didanosine and nevirapine. | 2001-07-06 |
|
| A pilot trial of indinavir, ritonavir, didanosine, and lamivudine in a once-daily four-drug regimen for HIV infection. | 2001-07-01 |
|
| Antiretroviral-induced hepatic steatosis and lactic acidosis: case report and review of the literature. | 2001-07 |
|
| Gynaecomastia in a male patient during stavudine and didanosine treatment for HIV infection. | 2001-07 |
|
| Updated U.S. Public Health Service Guidelines for the Management of Occupational Exposures to HBV, HCV, and HIV and Recommendations for Postexposure Prophylaxis. | 2001-06-29 |
|
| High exposure to nevirapine in plasma is associated with an improved virological response in HIV-1-infected individuals. | 2001-06-15 |
|
| 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). | 2001-06-15 |
|
| [Symptomatic hyperlactemia in patients infected with the human immunodeficiency virus treated with nucleoside analogs]. | 2001-06-09 |
|
| Mitochondrial toxic effects and ribavirin. | 2001-06-02 |
|
| Mitochondrial toxic effects and ribavirin. | 2001-06-02 |
|
| A randomized, open-label, comparative trial of zidovudine plus lamivudine versus zidovudine plus lamivudine plus didanosine in antiretroviral-naive HIV-1-infected Thai patients. | 2001-06-01 |
|
| Nucleoside analogue-induced fatal lactic acidosis in two HIV-infected patients in Singapore. | 2001-06 |
|
| Full recovery from severe dilated cardiomyopathy in an HIV-infected patient. | 2001-06 |
|
| New developments in anti-HIV chemotherapy. | 2001-05-12 |
|
| Myelopathy in a previously asymptomatic HIV-1-infected patient. | 2001-05-08 |
|
| Fatal portal hypertension, liver failure, and mitochondrial dysfunction after HIV-1 nucleoside analogue-induced hepatitis and lactic acidaemia. | 2001-05-05 |
|
| HIV in body fluids during primary HIV infection: implications for pathogenesis, treatment and public health. | 2001-05-04 |
|
| [HIV-HBV coinfection and the liver]. | 2001-05 |
|
| Choosing which nuke to use first. | 2001-05 |
|
| High prevalence of genotypic and phenotypic HIV-1 drug-resistant strains among patients receiving antiretroviral therapy in Abidjan, Côte d'Ivoire. | 2001-04-15 |
|
| A pilot study of the use of mycophenolate mofetil as a component of therapy for multidrug-resistant HIV-1 infection. | 2001-04-15 |
|
| Differing reverse transcriptase mutation patterns in individuals experiencing viral rebound on first-line regimens with stavudine/didanosine and stavudine/lamivudine. | 2001-04-13 |
|
| Determination of serum levels of thirteen human immunodeficiency virus-suppressing drugs by high-performance liquid chromatography. | 2001-04-13 |
|
| [Didanosine as a capsule. A reliable drug in a new dosage form]. | 2001-04-02 |
|
| [A rare etiology of hepatic steatosis associated with lactic acidosis: the toxicity of antiviral nucleoside analogues]. | 2001-04 |
|
| Smaller amounts of antiretroviral drugs are needed when combined with an active ribozyme against HIV-1. | 2001-04 |
|
| Vertical HIV-1 transmission: prophylaxis and paediatric follow-up. | 2001-04 |
|
| An open-label randomized trial to evaluate different therapeutic strategies of combination therapy in HIV-1 infection: design, rationale, and methods of the initio trial. | 2001-04 |
|
| Incidence of pancreatitis in HIV-infected patients receiving nucleoside reverse transcriptase inhibitor drugs. | 2001-03-30 |
|
| Mutations in the non-nucleoside binding-pocket interfere with the multi-nucleoside resistance phenotype. | 2001-03-30 |
|
| Differential susceptibility of retroviruses to nucleoside analogues. | 2001-03 |
|
| Virological response in multidrug-experienced HIV-1-infected subjects failing highly active combination regimens after shifting from lamivudine to didanosine. | 2001-03 |
|
| Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent. | 2001-02-01 |
|
| Clinical and laboratory signs of mitochondrial dysfunction secondary to nucleoside analogue antiretroviral therapy are reversible. | 2001 |
|
| HIV-1 multi-dideoxynucleoside resistance mutation (Q151M): prevalence, associated resistance mutations and response to antiretroviral salvage treatment. | 2001 |
|
| Delavirdine: clinical pharmacokinetics and drug interactions. | 2001 |
Sample Use Guides
In adult patients didanosine should be administered on an empty stomach at least 30 minutes before eating at the dose of 200 mg twice daily (body weight is at least 60 kg) or 125 mg twice daily (body weight is less than 60 kg). Pediatric patients (2 weeks old to 18 years old): the drug should be administered on an empty stomach at least 30 minutes before or 2 hours after eating at the dose of 100-120 mg per m2 twice daily.
Route of Administration:
Oral
The anti-HIV-1 activity of didanosine was evaluated in a variety of HIV-1 infected lymphoblastic cell lines and monocyte/macrophage cell cultures. The concentration of drug necessary to inhibit viral replication by 50% (EC50) ranged from 2.5 to 10 uM (1 uM = 0.24 ug/mL) in lymphoblastic cell lines and 0.01 to 0.1 uM in monocyte/macrophage cell cultures.
| Substance Class |
Chemical
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| Record UNII |
K3GDH6OH08
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Validated (UNII)
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| Classification Tree | Code System | Code | ||
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NDF-RT |
N0000009947
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WHO-VATC |
QJ05AF02
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NDF-RT |
N0000175459
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NCI_THESAURUS |
C97452
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WHO-ATC |
J05AF02
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WHO-ESSENTIAL MEDICINES LIST |
6.4.2.1
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NDF-RT |
N0000175459
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FDA ORPHAN DRUG |
29488
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NDF-RT |
N0000175462
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NDF-RT |
N0000175459
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LIVERTOX |
NBK548326
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| Code System | Code | Type | Description | ||
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m4379
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PRIMARY | Merck Index | ||
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SUB07104MIG
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6548
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135398739
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DTXSID6022927
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K3GDH6OH08
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C431
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DIDANOSINE
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1191204
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6664
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Didanosine
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CHEMBL1460
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3364
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K3GDH6OH08
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100000087146
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69655-05-6
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D016049
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869
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4833
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DIDANOSINE
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PRIMARY | Description: A white to almost white powder.Solubility: Sparingly soluble in water; slightly soluble in methanol R and ethanol (95 per cent) R.Category: Antiretroviral (Nucleoside Reverse Transcriptase Inhibitor).Storage: Didanosine should be kept in a tightly closed container.Requirements: Didanosine contains not less than 98.5% and not more than 101.0% of C10H12N4O3, calculated with reference to the driedsubstance. | ||
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612049
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CC-20
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490877
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DB00900
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
USP
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (TITRATION)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT | |||
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IMPURITY -> PARENT | |||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT | |||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT | |||
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IMPURITY -> PARENT | |||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT | |||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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ACTIVE MOIETY |
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