Punit Marathe

Summary

Affiliation: Bristol-Myers Squibb
Country: USA

Publications

  1. ncbi request reprint Selective Itk inhibitors block T-cell activation and murine lung inflammation
    Tai an Lin
    Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543, USA
    Biochemistry 43:11056-62. 2004
  2. ncbi request reprint Development and validation of a preclinical food effect model
    Kimberley 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
  3. doi request reprint Examination of CYP3A and P-glycoprotein-mediated drug-drug interactions using animal models
    Punit H Marathe
    Metabolism and Pharmacokinetics, Bristol Myers Squibb, Pennington, NJ, USA
    Methods Mol Biol 596:385-403. 2010
  4. ncbi request reprint In vivo animal models for investigating potential CYP3A- and Pgp-mediated drug-drug interactions
    Punit H Marathe
    Metabolism and Pharmacokinetics, Bristol Myers Squibb, Princeton, NJ 08543, USA
    Curr Drug Metab 7:687-704. 2006
  5. doi request reprint Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2
    Punit Marathe
    Department of Metabolism and Pharmacokinetics, Bristol Myers Squibb Company, Princeton, New Jersey, USA
    J Pharm Sci 99:3579-93. 2010
  6. doi request reprint Preclinical pharmacokinetics and in vitro metabolism of brivanib (BMS-540215), a potent VEGFR2 inhibitor and its alanine ester prodrug brivanib alaninate
    Punit H Marathe
    Pharmaceutical Candidate Optimization, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08540, USA
    Cancer Chemother Pharmacol 65:55-66. 2009
  7. ncbi request reprint 5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases
    Harold 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
  8. doi request reprint 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 fa
    Zhen Wei Cai
    Bristol Myers Squibb Research and Development, Princeton, NJ 08543, USA
    J Med Chem 51:1976-80. 2008
  9. ncbi request reprint 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 agent
    Raj N Misra
    Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, New Jersey 08543 4000, USA
    J Med Chem 47:1719-28. 2004
  10. doi request reprint 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 epider
    Ashvinikumar V Gavai
    Bristol Myers Squibb Research and Development, P O Box 4000, Princeton, New Jersey 08543, USA
    J Med Chem 52:6527-30. 2009

Detail Information

Publications35

  1. ncbi request reprint Selective Itk inhibitors block T-cell activation and murine lung inflammation
    Tai 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...
  2. ncbi request reprint Development and validation of a preclinical food effect model
    Kimberley 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...
  3. doi request reprint Examination of CYP3A and P-glycoprotein-mediated drug-drug interactions using animal models
    Punit 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...
  4. ncbi request reprint In vivo animal models for investigating potential CYP3A- and Pgp-mediated drug-drug interactions
    Punit 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...
  5. doi request reprint Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2
    Punit 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...
  6. doi request reprint Preclinical pharmacokinetics and in vitro metabolism of brivanib (BMS-540215), a potent VEGFR2 inhibitor and its alanine ester prodrug brivanib alaninate
    Punit 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...
  7. ncbi request reprint 5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases
    Harold 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...
  8. doi request reprint 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 fa
    Zhen 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...
  9. ncbi request reprint 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 agent
    Raj 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...
  10. doi request reprint 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 epider
    Ashvinikumar 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...
  11. doi request reprint Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities
    Kyoung 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...
  12. ncbi request reprint 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 inhibitor
    Rajeev 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...
  13. ncbi request reprint 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-2
    Robert 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...
  14. ncbi request reprint Novel C-5 aminomethyl pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases
    Harold 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...
  15. doi request reprint Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors
    Zhen 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...
  16. doi request reprint 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 extrapolation
    Hong 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...
  17. ncbi request reprint 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...
  18. doi request reprint Development of a canine model to enable the preclinical assessment of pH-dependent absorption of test compounds
    R 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...
  19. doi request reprint A liquid chromatography tandem mass spectrometry method for the quantification of indocyanine green in dog plasma and bile
    Cliff 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)...
  20. doi request reprint 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)nicotin
    Scott 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...
  21. ncbi request reprint Steady-state pharmacokinetics of a novel extended-release metformin formulation
    Peter 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...
  22. ncbi request reprint New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases
    Harold 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...
  23. ncbi request reprint Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors
    Jagabandhu Das
    Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543 4000, USA
    Bioorg Med Chem Lett 16:3706-12. 2006
    ....
  24. pmc Factors influencing magnitude and duration of target inhibition following antibody therapy: implications in drug discovery and development
    Anjaneya P Chimalakonda
    Metabolism and Pharmacokinetics, Department of Pharmaceutical Candidate Optimization, Bristol Myers Squibb Co, Mail Stop 17 2 04, Pennington, NJ 08534, USA
    AAPS J 15:717-27. 2013
    ..The implications of these simulations in drug discovery and development with regard to target identification, antibody optimization, and backup candidate selection are discussed. ..
  25. doi request reprint Cytochrome P450 11A1 bioactivation of a kinase inhibitor in rats: use of radioprofiling, modulation of metabolism, and adrenocortical cell lines to evaluate adrenal toxicity
    Donglu 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...
  26. ncbi request reprint Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities
    Kyoung 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
    ....
  27. ncbi request reprint 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 assays
    Louis 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...
  28. doi request reprint 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 inhibitor
    John 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...
  29. ncbi request reprint P-glycoprotein plays a role in the oral absorption of BMS-387032, a potent cyclin-dependent kinase 2 inhibitor, in rats
    Amrita 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...
  30. ncbi request reprint Preclinical pharmacokinetics and oral bioavailability of BMS-310705, a novel epothilone B analog
    Amrita 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...
  31. ncbi request reprint Novel fluoro-substituted camptothecins: in vivo antitumor activity, reduced gastrointestinal toxicity and pharmacokinetic characterization
    William 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...
  32. ncbi request reprint Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL
    Amrita 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...
  33. ncbi request reprint Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors
    John 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...
  34. doi request reprint Benzothiazole based inhibitors of p38alpha MAP kinase
    Chunjian 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...
  35. ncbi request reprint Effect of commonly used organic solvents on the kinetics of cytochrome P450 2B6- and 2C8-dependent activity in human liver microsomes
    Ragini 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...