Compounds > bms-275183
Page last updated: 2024-12-11

bms-275183

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

BMS-275183: an orally active taxane in Phase I clinical trials (10/2001) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6918594
CHEMBL ID4297268
SCHEMBL ID13900214
MeSH IDM0402249

Synonyms (10)

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

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" 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)		0.58
" 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)		0.58
" 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)		0.58

Bioavailability

ExcerptReferenceRelevance
"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)		0.66
"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, )		3.02

Dosage Studied

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.

ExcerptRelevanceReference
" 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)		0.58
" BMS-275183 can be given orally by flat dosing instead of BSA-normalized dosing."( 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)		1.49
" 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 of BMS-275183 on a daily dosing schedule."( A phase 1 study of BMS-275183, a novel oral analogue of paclitaxel given on a daily schedule to patients with advanced malignancies.
Alland, L; Awada, A; Belani, CP; Besse-Hamer, T; Cardoso, F; Egorin, MJ; Has, T; Heath, EI; Lorusso, P; Ramalingam, SS; Valdivieso, M; Zhou, X, 2011)		0.89
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's9 (81.82)29.6817
2010's2 (18.18)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.45

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.

MetricThis Compound (vs All)
Research Demand Index11.45 (24.57)
Research Supply Index2.83 (2.92)
Research Growth Index4.29 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.45)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (33.33%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (66.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
pantoprazole
Pantoprazole: 2-pyridinylmethylsulfinylbenzimidazole proton pump inhibitor that is used in the treatment of GASTROESOPHAGEAL REFLUX and PEPTIC ULCER.. pantoprazole : A member of the class of benzimidazoles that is 1H-benzimidazole substituted by a difluoromethoxy group at position 5 and a [(3,4-dimethoxypyridin-2-yl)methyl]sulfinyl group at position 2.		2.110aromatic ether;
benzimidazoles;
organofluorine compound;
pyridines;
sulfoxide		anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
environmental contaminant;
xenobiotic
paclitaxel
Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).		2.7230taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
epothilone b
[no description available]		2.0110epothilone;
epoxide		antineoplastic agent;
apoptosis inducer;
microtubule-stabilising agent
epothilone a
Epothilones: A group of 16-member MACROLIDES which stabilize MICROTUBULES in a manner similar to PACLITAXEL. They were originally found in the myxobacterium Sorangium cellulosum, now renamed to Polyangium (MYXOCOCCALES).		2.0110epothilone;
epoxide		antineoplastic agent;
metabolite;
microtubule-stabilising agent;
tubulin modulator
ly335979
[no description available]		2.110carbopolycyclic compound
perfosfamide
[no description available]		2.0110
taxane
taxane: produced by Taxomyces andreanae		7.0110diterpene;
terpenoid fundamental parent
ConditionIndicatedRelationship StrengthStudiesTrials
Blood Poisoning
[description not available]		03.4511
Benign Neoplasms
[description not available]		05.2543
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		17.2543
Neutropenia
A decrease in the number of NEUTROPHILS found in the blood.		04.3922
Sepsis
Systemic inflammatory response syndrome with a proven or suspected infectious etiology. When sepsis is associated with organ dysfunction distant from the site of infection, it is called severe sepsis. When sepsis is accompanied by HYPOTENSION despite adequate fluid infusion, it is called SEPTIC SHOCK.		03.4511
Breast Cancer
[description not available]		02.0110
Breast Neoplasms
Tumors or cancer of the human BREAST.		02.0110
Experimental Neoplasms
[description not available]		02.4220
Carcinoma, Non-Small Cell Lung
[description not available]		03.4111
Cancer of Colon
[description not available]		03.4111
Lassitude
[description not available]		03.4111
Cancer of Lung
[description not available]		03.4111
Ache
[description not available]		03.4111
Carcinoma, Non-Small-Cell Lung
A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.		15.4111
Colonic Neoplasms
Tumors or cancer of the COLON.		03.4111
Fatigue
The state of weariness following a period of exertion, mental or physical, characterized by a decreased capacity for work and reduced efficiency to respond to stimuli.		03.4111
Lung Neoplasms
Tumors or cancer of the LUNG.		03.4111
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		03.4111