Page last updated: 2024-12-08
raluridine
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
raluridine: inhibitor of HIV; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 451480 |
| CHEMBL ID | 2106991 |
| SCHEMBL ID | 419653 |
| MeSH ID | M0165994 |
Synonyms (34)
| Synonym |
|---|
| 935u-83 |
| raluridine (usan) |
| D05695 |
| bw 935u83 |
| 5clu: |
| 5-chloro-1-[(2r,4s,5r)-4-fluoro-5-(hydroxymethyl)tetrahydrofuran-2-yl]pyrimidine-2,4-dione |
| 2',3'-dideoxy-3'-fluoro-5-chlorouridine |
| 119644-22-3 |
| raluridine |
| fddclu |
| 5-chloro-1-[(2r,4s,5r)-4-fluoro-5-(hydroxymethyl)oxolan-2-yl]pyrimidine-2,4-dione |
| 5-chloro-2',3'-dideoxy-3'-fluoro-uridine |
| 935-u-83 |
| CHEMBL2106991 |
| 3'-fluoro-2',3'-dideoxy-5-chlorouridine |
| fddciu |
| 935u83 |
| 5-chloro-2',3'-dideoxy-3'-fluorouridine |
| unii-9d65nwy2k0 |
| fddclurd |
| 9d65nwy2k0 , |
| uridine, 5-chloro-2',3'-dideoxy-3'-fluoro- |
| drg-0215 |
| raluridine [usan] |
| SCHEMBL419653 |
| raluridine [who-dd] |
| AC-32302 |
| DTXSID30152541 |
| AKOS030568062 |
| DB12894 |
| 5-chloro-1-((2r,4s,5r)-4-fluoro-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidine-2,4(1h,3h)-dione |
| WKVDSZYIGHLONN-RRKCRQDMSA-N |
| 5-chloro-3'-fluoro-2',3'-dideoxyuridine |
| Q27272384 |
Research Excerpts
Toxicity
| Excerpt | Reference | Relevance |
|---|---|---|
| " In the dose range of 100 to 1,500 mg 935U83 was well tolerated by all subjects with no drug-related adverse events reported." | ( Safety and pharmacokinetics of 5-chloro-2',3'-dideoxy-3'-fluorouridine (935U83) following oral administration of escalating single doses in human immunodeficiency virus-infected adults. Bartlett, JA; Blum, MR; Dunn, JA; Elkins, MM; McMahon, DK; Mellors, JW; Packard, MV; Riddler, SA; Savina, PM; Wang, LH, 1996) | 0.29 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| " Pharmacokinetic evaluation showed good oral bioavailability (86% in mice and 60% in monkeys) and less extensive metabolism to the glucuronide relative to AZT." | ( 5-Chloro-2',3'-dideoxy-3'-fluorouridine (935U83), a selective anti-human immunodeficiency virus agent with an improved metabolic and toxicological profile. Ayers, KM; Daluge, SM; Dev, IK; Novak, P; Parry, NR; Purifoy, DJ; Reardon, JE; Roberts, GB; Savina, PM; St Clair, MH, 1994) | 0.29 |
| " The effect of a high-fat meal on the oral bioavailability of 935U83 was also assessed." | ( Safety and pharmacokinetics of 5-chloro-2',3'-dideoxy-3'-fluorouridine (935U83) following oral administration of escalating single doses in human immunodeficiency virus-infected adults. Bartlett, JA; Blum, MR; Dunn, JA; Elkins, MM; McMahon, DK; Mellors, JW; Packard, MV; Riddler, SA; Savina, PM; Wang, LH, 1996) | 0.29 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " Mild reversible reductions in erythrocytes and associated parameters were seen in mice dosed orally with 2,000 mg of 935U83 per kg per day for 1 and 6 months." | ( 5-Chloro-2',3'-dideoxy-3'-fluorouridine (935U83), a selective anti-human immunodeficiency virus agent with an improved metabolic and toxicological profile. Ayers, KM; Daluge, SM; Dev, IK; Novak, P; Parry, NR; Purifoy, DJ; Reardon, JE; Roberts, GB; Savina, PM; St Clair, MH, 1994) | 0.29 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (1)
Other Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | ED50 | 0.3800 | 0.0002 | 0.9935 | 9.8000 | AID105582 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Bioassays (10)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID235486 | Selectivity index is the ratio of ED50 and CD50 values against inhibition of HIV-1 in MT-4 cells | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 3'-Fluoro-2',3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'- and 3'-fluorinated 2',3'-dideoxynucleoside analogues. |
| AID1652588 | Cytotoxicity in human CEM/0 cells assessed as reduction in cell viability incubated for 4 to 5 days | |||
| AID104310 | Effective dose achieving 50% protection of MT-4 cells against the cytopathic effect of HIV | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Synthesis and anti-HIV evaluation of 2',3'-dideoxyribo-5-chloropyrimidine analogues: reduced toxicity of 5-chlorinated 2',3'-dideoxynucleosides. |
| AID1652587 | Antiviral activity against HIV2 ROD infected in human TK-deficient CEM/TK(-) cells assessed as inhibition of viral-induced giant cell formation incubated for 4 to 5 days by microscopy | |||
| AID235704 | Selectivity index of CD50 to ED50 of MT-4 cells | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Synthesis and anti-HIV evaluation of 2',3'-dideoxyribo-5-chloropyrimidine analogues: reduced toxicity of 5-chlorinated 2',3'-dideoxynucleosides. |
| AID105582 | Inhibitory activity against HIV-1 replication in MT-4 cells | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 3'-Fluoro-2',3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'- and 3'-fluorinated 2',3'-dideoxynucleoside analogues. |
| AID106768 | Cytotoxic dose required to reduce the viability of normal uninfected MT-4 cells by 50% | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | Synthesis and anti-HIV evaluation of 2',3'-dideoxyribo-5-chloropyrimidine analogues: reduced toxicity of 5-chlorinated 2',3'-dideoxynucleosides. |
| AID1652585 | Antiviral activity against HIV1 3B infected in human CEM/0 cells assessed as inhibition of viral-induced giant cell formation incubated for 4 to 5 days by microscopy | |||
| AID105376 | Cytotoxic dose in MT-4 cells | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 3'-Fluoro-2',3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'- and 3'-fluorinated 2',3'-dideoxynucleoside analogues. |
| AID1652586 | Antiviral activity against HIV2 ROD infected in human CEM/0 cells assessed as inhibition of viral-induced giant cell formation incubated for 4 to 5 days by microscopy | |||
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (8)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 2 (25.00) | 18.7374 |
| 1990's | 5 (62.50) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 1 (12.50) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 12.39
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (12.39) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (12.50%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 7 (87.50%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||