BMS-275183: an orally active taxane in Phase I clinical trials (10/2001) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 6918594 |
| CHEMBL ID | 4297268 |
| SCHEMBL ID | 13900214 |
| MeSH ID | M0402249 |
| Synonym |
|---|
| bms-275183 |
| uqc681jjiv , |
| unii-uqc681jjiv |
| 355113-98-3 |
| bms 275183 [who-dd] |
| SCHEMBL13900214 |
| DB12144 |
| Q27291199 |
| CHEMBL4297268 |
| [(1s,2s,3r,4s,7r,9s,10s,12r,15s)-12-acetyloxy-1,9-dihydroxy-15-[(2r,3s)-2-hydroxy-4,4-dimethyl-3-[(2-methylpropan-2-yl)oxycarbonylamino]pentanoyl]oxy-4-methoxycarbonyloxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-en-2-yl |
| Excerpt | Reference |
|---|---|
| " Additionally, we evaluated its pharmacokinetic variability using flat-fixed dosing compared with dosing individualized by body surface area (BSA)." | ( Effect of food on the pharmacokinetic behavior of the potent oral taxane BMS-275183. Bröker, LE; Deluca, P; Giaccone, G; Lorusso, PM; Parker, S; Pilat, MJ; Valdivieso, M; Zhou, X, 2008) |
| " Pharmacokinetic sampling was done up to 72 hours after the first four doses and analyzed with a validated liquid chromatography/mass spectrometry assay." | ( Effect of food on the pharmacokinetic behavior of the potent oral taxane BMS-275183. Bröker, LE; Deluca, P; Giaccone, G; Lorusso, PM; Parker, S; Pilat, MJ; Valdivieso, M; Zhou, X, 2008) |
| " Pharmacokinetic data were available for 26 patients (A and C), 24 patients (B), and 21 patients (D)." | ( Effect of food on the pharmacokinetic behavior of the potent oral taxane BMS-275183. Bröker, LE; Deluca, P; Giaccone, G; Lorusso, PM; Parker, S; Pilat, MJ; Valdivieso, M; Zhou, X, 2008) |
| Excerpt | Reference |
|---|---|
| "The evolution of 2, a C-4-methylcarbonate analogue of paclitaxel with minimal oral bioavailability and oral efficacy, into its C-3'-t-butyl-3'-N-t-butyloxycarbonyl analogue (15i), a novel taxane with oral efficacy in preclinical models that is comparable to iv administered paclitaxel, is described." | ( The discovery of BMS-275183: an orally efficacious novel taxane. Cook, D; Fairchild, CR; Hansel, S; Johnson, W; Kadow, JF; Long, BH; Mastalerz, H; Rose, WC; Tarrant, J; Vyas, DM; Wu, MJ; Xue, MQ; Zhang, G; Zoeckler, M, 2003) |
| "BMS-275183 is an orally bioavailable taxane that has antitumor activity in preclinical cancer models." | ( BMS-275183-induced gene expression patterns in head and neck carcinoma. Ensley, JF; Ezzat, WH; Kim, H; Lemonnier, LA; Lin, HS; Lonardo, F; Piechocki, MP; Subramanian, G; Tran, VR; Yoo, GH, ) |
BMS-275183 can be given orally by flat dosing instead of BSA-normalized dosing. The lack of evidence of clinical benefit and the occurrence of two fatal events of neutropenic sepsis, coupled with high drug exposure, argues against further evaluation.
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 9 (81.82) | 29.6817 |
| 2010's | 2 (18.18) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 4 (33.33%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 8 (66.67%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||