Research Topics
Genomes and GenesSpecies | Punit MaratheSummaryAffiliation: Bristol-Myers Squibb Country: USA Publications
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Publications
Selective Itk inhibitors block T-cell activation and murine lung inflammationTai an Lin
Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543, USA
Biochemistry 43:11056-62. 2004..Our findings represent the first description of selective inhibitors to probe human Itk function and its associated pathway, and support the hypothesis that Itk is a therapeutic target for immunosuppressive and inflammatory diseases...- Development and validation of a preclinical food effect modelKimberley A Lentz
Pharmaceutical Candidate Optimization, Metabolism and Pharmacokinetics, Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, Connecticut 06492 1951, USA
J Pharm Sci 96:459-72. 2007..This model, which is intended for compound screening, will be helpful for determining food effect as a liability when compounds progress from discovery to clinical development... 
Examination of CYP3A and P-glycoprotein-mediated drug-drug interactions using animal modelsPunit H Marathe
Metabolism and Pharmacokinetics, Bristol Myers Squibb, Pennington, NJ, USA
Methods Mol Biol 596:385-403. 2010..Such an integrated data set can be used to select drug candidates with a reduced DDI potential...- In vivo animal models for investigating potential CYP3A- and Pgp-mediated drug-drug interactionsPunit H Marathe
Metabolism and Pharmacokinetics, Bristol Myers Squibb, Princeton, NJ 08543, USA
Curr Drug Metab 7:687-704. 2006..Such an integrated data set can be used to select drug candidates with a reduced drug interaction potential... - Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2Punit Marathe
Department of Metabolism and Pharmacokinetics, Bristol Myers Squibb Company, Princeton, New Jersey, USA
J Pharm Sci 99:3579-93. 2010..Based on the efficacious AUC in nude mice and predicted human pharmacokinetics, the human efficacious QD dose is predicted to be in the range of 100-200 mg... - Preclinical pharmacokinetics and in vitro metabolism of brivanib (BMS-540215), a potent VEGFR2 inhibitor and its alanine ester prodrug brivanib alaninatePunit H Marathe
Pharmaceutical Candidate Optimization, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08540, USA
Cancer Chemother Pharmacol 65:55-66. 2009..In vitro and in vivo studies were conducted to characterize the preclinical pharmacokinetics and disposition of brivanib and brivanib alaninate, and antitumor efficacy in mice bearing human xenografts... - 5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinasesHarold Mastalerz
Department of Oncology Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492 1951, USA
Bioorg Med Chem Lett 17:4947-54. 2007..It is hypothesized that this solubilizing group extends into the ribose-phosphate portion of the ATP binding pocket and enhances the binding affinity of the inhibitor... - Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth faZhen Wei Cai
Bristol Myers Squibb Research and Development, Princeton, NJ 08543, USA
J Med Chem 51:1976-80. 2008..The l-alanine prodrug 8 (also known as brivanib alaninate/BMS-582664) was selected as a development candidate and is presently in phase II clinical trials... - N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agentRaj N Misra
Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, New Jersey 08543 4000, USA
J Med Chem 47:1719-28. 2004..c./i.p. A2780 human ovarian carcinoma xenograft model... - Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epiderAshvinikumar V Gavai
Bristol Myers Squibb Research and Development, P O Box 4000, Princeton, New Jersey 08543, USA
J Med Chem 52:6527-30. 2009..On the basis of its favorable pharmacokinetic profile and robust in vivo activity in HER1 and HER2 driven tumor models, 13 (BMS-599626) was selected as a clinical candidate for treatment of solid tumors... - Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activitiesKyoung Soon Kim
Department of Oncology Chemistry, Bristol Myers Squibb Pharmaceutical Research and Development, P O Box 4000, Princeton, New Jersey 08543 4000, USA
J Med Chem 51:5330-41. 2008..It possesses a favorable pharmacokinetic profile in mice and demonstrates significant in vivo antitumor activity in the GTL-16 human gastric carcinoma xenograft model... - Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitorRajeev S Bhide
Bristol Myers Squibb, Pharmaceutical Research Institute, Princeton, New Jersey 08543 4000, USA
J Med Chem 49:2143-6. 2006..The l-alanine prodrug of 12, BMS-582664 (21), is currently under evaluation in clinical trials for the treatment of solid tumors... - Novel C-5 aminomethyl pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinasesHarold Mastalerz
Department of Oncology Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492 1951, USA
Bioorg Med Chem Lett 17:2828-33. 2007..It is hypothesized that the C-5 homopiperazine side chain binds in the ribose-phosphate portion of the ATP binding pocket... - Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2Robert M Borzilleri
Bristol Myers Squibb Pharmaceutical Research Institute, P O Box 4000, Princeton, New Jersey 08543 4000, USA
J Med Chem 49:3766-9. 2006..Analogue 14 demonstrated excellent kinase selectivity, favorable pharmacokinetic properties in multiple species, and robust in vivo efficacy in human lung and colon carcinoma xenograft models... - Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitorsZhen Wei Cai
Bristol Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 18:3224-9. 2008..These studies led to the discovery of compounds 3b and 20b, which demonstrated favorable pharmacokinetic properties in mice and significant antitumor activity in a human gastric carcinoma xenograft model... - Projection of exposure and efficacious dose prior to first-in-human studies: how successful have we been?Christine Huang
Metabolism and Pharmacokinetics, Pharmaceutical Candidate Optimization, Bristol Myers Squibb Co, PO Box 5400, Princeton, New Jersey 08543 5400, USA
Pharm Res 25:713-26. 2008..In each case, exposure and efficacy in human subjects were projected at the time of nomination (for development) prior to first-in-human dosing... - Development of a canine model to enable the preclinical assessment of pH-dependent absorption of test compoundsR Marcus Fancher
Pharmaceutical Candidate Optimization Metabolism and Pharmacokinetics, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08540, USA
J Pharm Sci 100:2979-88. 2011..The model described herein can be used preclinically to screen out compounds, differentiate compounds, and support the assessment of various formulation- and prodrug-based strategies to mitigate the pH effect... - A liquid chromatography tandem mass spectrometry method for the quantification of indocyanine green in dog plasma and bileCliff Y Chen
Metabolism and Pharmacokinetics, Pharmaceutical Candidate Optimization, Bristol Myers Squibb Co, Princeton, NJ 08543, USA
J Pharm Biomed Anal 47:351-9. 2008..The method described herein is sensitive, selective and faster than other existing methods (e.g., spectrophotometry, HPLC/UV-vis detection, or HPLC/fluorescence detection)... - New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinasesHarold Mastalerz
Department of Oncology Chemistry, 5 Research Parkway, Wallingford, CT 06492 1951, USA
Bioorg Med Chem Lett 17:2036-42. 2007..The lead compound exhibited promising oral efficacy in both EGFR and HER2 driven human tumor xenograft models. It is hypothesized that its C-5 morpholine side chain binds in the ribose phosphate portion of the ATP binding pocket... - Steady-state pharmacokinetics of a novel extended-release metformin formulationPeter Timmins
Bristol Myers Squibb Company, Pharmaceutical Research Institute, Moreton, UK
Clin Pharmacokinet 44:721-9. 2005..The objective of this study was to assess the steady-state pharmacokinetics of metformin XR tablets... - Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinScott H Watterson
Bristol Myers Squibb Research and Development, P O Box 4000, Princeton, New Jersey 08543, USA
J Med Chem 53:3814-30. 2010..4]nonan-7-yl)nicotinic acid (2e) was selected to advance into clinical trials... - Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitorsJagabandhu Das
Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 16:3706-12. 2006.... - Cytochrome P450 11A1 bioactivation of a kinase inhibitor in rats: use of radioprofiling, modulation of metabolism, and adrenocortical cell lines to evaluate adrenal toxicityDonglu Zhang
Department of Pharmaceutical Candidate Optimization, Bristol Myers Squibb Research and Development, Princeton, New Jersey 08543, USA
Chem Res Toxicol 25:556-71. 2012..The thorough understanding of the metabolism-dependent adrenal toxicity was useful to evaluate cross-species adrenal toxicity potential of this compound and related analogues... - Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assaysLouis J Lombardo
Bristol Myers Squibb Pharmaceutical Research Institute, P O Box 4000, Princeton, New Jersey 08543 4000, USA
J Med Chem 47:6658-61. 2004..On the basis of its robust in vivo activity and favorable pharmacokinetic profile, 13 was selected for additional characterization for oncology indications... - Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activitiesKyoung Soon Kim
Department of Oncology Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543 4000, USA
J Med Chem 45:3905-27. 2002.... - Cynomolgus monkey as a potential model to assess drug interactions involving hepatic organic anion transporting polypeptides: in vitro, in vivo, and in vitro-to-in vivo extrapolationHong Shen
Department of Pharmaceutical Candidate Optimization, Bristol Myers Squibb Research and Development, Princeton, New Jersey, USA
J Pharmacol Exp Ther 344:673-85. 2013..It is concluded that the cynomolgus monkey has the potential to serve as a useful model for the assessment of OATP-mediated DDIs in a nonclinical setting... - The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitorJohn Hynes
Bristol Myers Squibb, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 18:1762-7. 2008..Optimization of the lead series generated 6e, BMS-640994, a potent and selective p38alpha inhibitor that is orally efficacious in rodent models of acute and chronic inflammation... - P-glycoprotein plays a role in the oral absorption of BMS-387032, a potent cyclin-dependent kinase 2 inhibitor, in ratsAmrita V Kamath
Department of Metabolism and Pharmacokinetics, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA
Cancer Chemother Pharmacol 55:110-6. 2005..The oral bioavailability of BMS-387032 has been found to be about 31% in rats. Absorption and first-pass metabolism were evaluated as possible reasons for the incomplete oral bioavailability in rats... - Preclinical pharmacokinetics and oral bioavailability of BMS-310705, a novel epothilone B analogAmrita V Kamath
Department of Metabolism and Pharmacokinetics, Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543, USA
Cancer Chemother Pharmacol 56:145-53. 2005..The in vitro and in vivo pharmacokinetics and oral bioavailability of BMS-310705 were investigated in mice, rats, and dogs. In addition, comparison of the pharmacokinetics of BMS-310705 using various formulations was conducted in rats... - Novel fluoro-substituted camptothecins: in vivo antitumor activity, reduced gastrointestinal toxicity and pharmacokinetic characterizationWilliam C Rose
Pharmaceutical Research Institute, Bristol Myers Squibb Co, Inc, Lawrenceville, NJ, USA
Cancer Chemother Pharmacol 58:73-85. 2006..The novel fluoro-substituted camptothecin analog, BMS-286309, and its prodrug, BMS-422461, were evaluated for their pharmacologic, toxicologic, metabolic and pharmacokinetic developmental potential... - Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABLAmrita V Kamath
Department of Pharmacokinetic and Pharmacodynamic Sciences, Genentech, 1 DNA Way, South San Francisco, CA 94080, USA
Cancer Chemother Pharmacol 61:365-76. 2008..Possible mechanisms contributing to the incomplete oral bioavailability of dasatinib in animals were investigated... - Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitorsJohn Hynes
Department of Immunology Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543 4000, USA
J Med Chem 51:4-16. 2008..In rodent disease models of chronic inflammation, multiple compounds demonstrated significant inhibition of disease progression leading to the advancement of 2 compounds 11b and 11j into further preclinical and toxicological studies... - Benzothiazole based inhibitors of p38alpha MAP kinaseChunjian Liu
Bristol Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 18:1874-9. 2008..The proposed binding mode of this new class of p38alpha inhibitors was confirmed by X-ray crystallographic studies of a representative inhibitor (6a) bound to the p38alpha enzyme... - Effect of commonly used organic solvents on the kinetics of cytochrome P450 2B6- and 2C8-dependent activity in human liver microsomesRagini Vuppugalla
Metabolism and Pharmacokinetics, Department of Pharmaceutical Candidate Optimization, Bristol Myer s Squibb Co, P O Box 4000, Princeton, NJ 08543, USA
Drug Metab Dispos 35:1990-5. 2007..Methanol and acetonitrile at concentrations of < or =0.5% and < or =1% (v/v) appeared to be suitable for the measurement of CYP2B6- and CYP2C8-mediated activities, respectively...