tucaresol: causes a dose-dependent left-shift of the oxygen saturation curve of hemoglobin S by stabilization of its oxy-(R)-conformation; an anti-sickling agent [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 55223 |
| CHEMBL ID | 2104482 |
| SCHEMBL ID | 600942 |
| MeSH ID | M0165817 |
| Synonym |
|---|
| tucaresol |
| 4-[(2-formyl-3-hydroxyphenoxy)methyl]benzoic acid |
| bw a589c |
| benzoic acid, 4-((2-formyl-3-hydroxyphenoxy)methyl)- |
| unii-jh368g5b9m |
| tucaresol [inn:ban] |
| bw-589c |
| jh368g5b9m , |
| bw 589c |
| alpha-(2-formyl-3-hydroxyphenoxy)-p-toluic acid |
| 589c80 |
| 589c |
| 84290-27-7 |
| 589-c |
| CHEMBL2104482 |
| benzoic acid, 4-[(2-formyl-3-hydroxyphenoxy)methyl]- |
| 4-[(2-formyl-3-hydroxy-phenoxy)methyl]benzoic acid |
| bwa 589c |
| SCHEMBL600942 |
| tucaresol [mart.] |
| .alpha.-(2-formyl-3-hydroxyphenoxy)-p-toluic acid |
| tucaresol [inn] |
| XEDONBRPTABQFB-UHFFFAOYSA-N |
| 4-(2-formyl-3-hydroxyphenoxymethyl) benzoic acid |
| 4-(2-formyl-3-hydroxyphenoxymethyl)benzoic acid |
| DTXSID70233247 |
| F9994-5209 |
| AKOS027327314 |
| DB13027 |
| 4-((2-formyl-3-hydroxyphenoxy)methyl)benzoic acid |
| 589c; 589c80; bwa 589c |
| E78089 |
| Q27281503 |
| BS-50680 |
| 4-[(2-formyl-3-hydroxyphenoxy)methyl]-benzoic acid |
| 4-((2-formyl-3-hydroxyphenoxy)methyl)benzoicacid |
Tucaresol is an orally administered antisickling agent. It increases the oxygen affinity of haemoglobin.
| Excerpt | Reference | Relevance |
|---|---|---|
| "1. Tucaresol is an orally administered antisickling agent which increases the oxygen affinity of haemoglobin. " | ( Pharmacokinetics and pharmacodynamics of tucaresol, an antisickling agent, in healthy volunteers. Mercer, AJ; Posner, J; Rolan, PE; Wootton, R, 1995) | 1.18 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Mean Cmax values in plasma and erythrocytes were 81." | ( Pharmacokinetics and pharmacodynamics of tucaresol, an antisickling agent, in healthy volunteers. Mercer, AJ; Posner, J; Rolan, PE; Wootton, R, 1995) | 0.56 |
| "There were no significant differences in standard pharmacokinetic parameters between the two occasions but the rate of tucaresol absorption was faster after food intake." | ( Effect of food and gender on the pharmacokinetics of tucaresol in healthy volunteers. Layton, G; Peck, RW; Posner, J; Wiggs, R; Wootton, R, 1998) | 0.76 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Tucaresol, which is orally bioavailable and systemically active, enhances CD4 Th-cell and CD8 cytotoxic T-cell responses in vivo and selectively favours a Th1-type profile of cytokine production." | ( Schiff base forming drugs: mechanisms of immune potentiation and therapeutic potential. Chen, H; Rhodes, J, 1996) | 1.2 |
The utility of tucaresol in the management of sickle cell disease will depend on the identification of a dosing regimen with a lower incidence of drug allergy. The acute increase in oxygen affinity is physiologically well-tolerated.
| Excerpt | Relevance | Reference |
|---|---|---|
| " The acute increase in oxygen affinity with tucaresol is physiologically well-tolerated, but the utility of tucaresol in the management of sickle cell disease will depend on the identification of a dosing regimen with a lower incidence of drug allergy." | ( Pharmacokinetics and pharmacodynamics of tucaresol, an antisickling agent, in healthy volunteers. Mercer, AJ; Posner, J; Rolan, PE; Wootton, R, 1995) | 0.82 |
| " Due to concerns over the sharp rise in haematocrit in one patient, subsequent cohorts received 300 mg tucaresol daily throughout the dosing period." | ( Tucaresol increases oxygen affinity and reduces haemolysis in subjects with sickle cell anaemia. Arya, R; Bellingham, AJ; Posner, J; Rolan, PE; Wootton, R, 1996) | 1.95 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1678657 | Immuno-adjuvant activity in E2deltaTM3-immunized BALB/cj mouse assessed as neutralization of HCV H77 genotype 1a pseudotyped virus particle with pooled immune sera at 1 ug/ml | 2020 | ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12 | Evaluation of a Series of Lipidated Tucaresol Adjuvants in a Hepatitis C Virus Vaccine Model. |
| AID1755546 | Clearance in human at 37 mg/kg, po by HPLC method | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients. |
| AID1755548 | Half life in human plasma at 37 mg/kg, po by HPLC method | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients. |
| AID1755540 | Cmax in human erythrocytes at 37 mg/kg, po | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients. |
| AID1755541 | Cmax in human plasma at 37 mg/kg, po by HPLC method | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients. |
| AID1755542 | Tmax in human erythrocytes at 37 mg/kg, po by HPLC method | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients. |
| AID1755547 | Half life in human erythrocytes at 37 mg/kg, po by HPLC method | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients. |
| AID1755545 | AUC (0 to 24 hrs) in human plasma at 37 mg/kg, po by HPLC method | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients. |
| AID1755539 | Ratio of drug level in human erythrocytes to plasma at 20 mg/kg, iv measured over 1 hr | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients. |
| AID1755544 | AUC (0 to 24 hrs) in human erythrocytes at 37 mg/kg, po by HPLC method | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients. |
| AID1755543 | Tmax in human plasma at 37 mg/kg, po by HPLC method | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 1 (3.85) | 18.7374 |
| 1990's | 12 (46.15) | 18.2507 |
| 2000's | 8 (30.77) | 29.6817 |
| 2010's | 3 (11.54) | 24.3611 |
| 2020's | 2 (7.69) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
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 moderate demand-to-supply ratio for research on this compound.
| This Compound (25.50) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 5 (19.23%) | 5.53% |
| Reviews | 4 (15.38%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 17 (65.38%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||