A. Kamath

发表

Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.

Punit Marathe, John S Tokarski, Toomas Mitt, 2002, Journal of medicinal chemistry.

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.

Ping Chen, A. Doweyko, Derek J. Norris, 2004, Journal of medicinal chemistry.

Preclinical pharmacokinetics of MEHD7945A, a novel EGFR/HER3 dual-action antibody, and prediction of its human pharmacokinetics and efficacious clinical dose

M. Sliwkowski, G. Schaefer, A. Kamath, 2012, Cancer Chemotherapy and Pharmacology.

Balancing the Affinity and Pharmacokinetics of Antibodies by Modulating the Size of Charge Patches on Complementarity-Determining Regions.

A. Kamath, Jinpian Diao, Zhilan Hu, 2020, Journal of pharmaceutical sciences.

Antibody Format and Serum Disposition Govern Ocular Pharmacokinetics of Intravenously Administered Protein Therapeutics

R. Kelley, A. Kamath, Hanine Rafidi, 2021, Frontiers in Pharmacology.

Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα).

C. Li, R. Rowntree, BinQing Wei, 2019, Bioorganic & medicinal chemistry letters.

Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.

J. Fargnoli, J. Barrish, J. Tokarski, 2005, Journal of medicinal chemistry.

Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.

Punit Marathe, Ravindra Tejwani, Arvind Mathur, 2008, Bioorganic & medicinal chemistry letters.

Metabolism of 5-Isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737): Identification of an Unusual N-Acetylglucosamine Conjugate in the Cynomolgus Monkey

Y. Shu, Donna D Wei, L. Qian, 2008, Drug Metabolism and Disposition.

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 factor receptor-1 kinase inhibitor (BMS-540215)

J. Fargnoli, G. Derbin, J. Barrish, 2008, Journal of medicinal chemistry.

Preclinical and translational pharmacokinetics of a novel THIOMAB™ antibody-antibiotic conjugate against Staphylococcus aureus

S. Ramanujan, A. Kamath, S. Sukumaran, 2019, mAbs.

Prediction of non-linear pharmacokinetics in humans of an antibody-drug conjugate (ADC) when evaluation of higher doses in animals is limited by tolerability: Case study with an anti-CD33 ADC

A. Kamath, K. Kozak, Keyang Xu, 2018, mAbs.

Pharmacokinetics and pharmacodynamics of DSTA4637A: A novel THIOMAB™ antibody antibiotic conjugate against Staphylococcus aureus in mice

S. Lehar, A. Kamath, C. Rosenberger, 2016, mAbs.

Preclinical pharmacokinetics of MHAA4549A, a human monoclonal antibody to influenza A virus, and the prediction of its efficacious clinical dose for the treatment of patients hospitalized with influenza A

Min Xu, A. Kamath, Summer Park, 2016, mAbs.

Dose dependent pharmacokinetics, tissue distribution, and anti-tumor efficacy of a humanized monoclonal antibody against DLL4 in mice

L. Khawli, Minhong Yan, S. Ross, 2014, mAbs.

Pharmacokinetics and Biodistribution of a Human Monoclonal Antibody to Oxidized LDL in Cynomolgus Monkey Using PET Imaging

S. Cherry, S. Rendig, C. Griesemer, 2012, PloS one.

Balancing Efficacy and Safety of an Anti-DLL4 Antibody through Pharmacokinetic Modulation

P. Hass, N. Lewin-Koh, J. Ridgway, 2015, Clinical Cancer Research.

Single cell-produced and in vitro-assembled anti-FcRH5/CD3 T-cell dependent bispecific antibodies have similar in vitro and in vivo properties

D. Danilenko, V. Plaks, P. Carter, 2018, mAbs.

Peripheral neuropathy with microtubule inhibitor containing antibody drug conjugates: Challenges and perspectives in translatability from nonclinical toxicology studies to the clinic.

A. Kamath, B. Fine, F. Brunstein, 2016, Regulatory toxicology and pharmacology : RTP.

Pharmacokinetics of Antibody–Drug Conjugates

A. Kamath, 2016 .

Challenges and advances in the assessment of the disposition of antibody‐drug conjugates

A. Kamath, S. Iyer, 2015, Biopharmaceutics & drug disposition.

Preclinical Pharmacokinetic Considerations for the Development of Antibody Drug Conjugates

A. Kamath, S. Iyer, 2014, Pharmaceutical Research.

Calicheamicin Antibody–Drug Conjugates with Improved Properties

B. Vollmar, A. Kamath, P. Dragovich, 2021, Molecular Cancer Therapeutics.

Modulating Therapeutic Activity and Toxicity of Pyrrolobenzodiazepine Antibody–Drug Conjugates with Self-Immolative Disulfide Linkers

Jeffrey T. Lau, S. Spencer, P. Polakis, 2017, Molecular Cancer Therapeutics.

Current Approaches for Absorption, Distribution, Metabolism, and Excretion Characterization of Antibody-Drug Conjugates: An Industry White Paper

D. Rock, Michaela Bairlein, A. Kamath, 2016, Drug Metabolism and Disposition.

Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors.

J. Fargnoli, J. Tokarski, J. Hunt, 2008, Bioorganic & medicinal chemistry letters.

A homogeneous high-DAR antibody–drug conjugate platform combining THIOMAB antibodies and XTEN polypeptides

R. Rowntree, A. Kamath, D. Reilly, 2021, Chemical science.

Anti-Ly6E-seco-CBI-Dimer Antibody-Drug Conjugate (ADC) That Forms Adduct with Alpha-1-microglobulin (A1M) Demonstrates Slower Systemic Antibody Clearance and Reduced Tumor Distribution in Animals

A. Kamath, Victor Yip, Carl Ng, 2020 .

Antibody-Drug Conjugates Derived from Cytotoxic seco-CBI-Dimer Payloads Are Highly Efficacious in Xenograft Models and Form Protein Adducts In Vivo.

Jeffrey T. Lau, R. Rowntree, B. Vollmar, 2019, Bioconjugate chemistry.

Effect of fruit juices on the oral bioavailability of fexofenadine in rats.

S. Chong, A. Kamath, Yueping Zhang, 2005, Journal of pharmaceutical sciences.

Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity

Melinda M. Mulvihill, Karen E Gascoigne, R. Rowntree, 2020, ChemMedChem.

Effect of molecular size on interstitial pharmacokinetics and tissue catabolism of antibodies

A. Kamath, G. Ferl, Hanine Rafidi, 2022, mAbs.

Selective Itk inhibitors block T-cell activation and murine lung inflammation.

A. Doweyko, S. Spergel, R. Moquin, 2004, Biochemistry.

Nonclinical Pharmacokinetics, Pharmacodynamics, and Translational Model of RO7297089, A Novel Anti-BCMA/CD16A Bispecific Tetravalent Antibody for the Treatment of Multiple Myeloma

Meric A. Ovacik, A. Kamath, A. Adedeji, 2022, The AAPS Journal.

Imaging Reveals Importance of Shape and Flexibility for Glomerular Filtration of Biologics

A. Estevez, Simon-Peter Williams, A. Kamath, 2021, Molecular Cancer Therapeutics.

Engineering Upper Hinge Improves Stability and Effector Function of a Human IgG1

B. Yan, P. Carter, G. Schaefer, 2011, The Journal of Biological Chemistry.

Minimal physiologically-based pharmacokinetic modeling of DSTA4637A, A novel THIOMAB™ antibody antibiotic conjugate against Staphylococcus aureus, in a mouse model

A. Kamath, Chenguang Zhou, C. Khojasteh, 2018, mAbs.

Sustained activity of novel THIOMAB antibody-antibiotic conjugate against Staphylococcus aureus in a mouse model: Longitudinal pharmacodynamic assessment by bioluminescence imaging

N. Lewin-Koh, A. Kamath, Chenguang Zhou, 2019, PloS one.

Nonclinical Pharmacokinetics and Pharmacodynamics Characterization of Anti-CD79b/CD3 T Cell-Dependent Bispecific Antibody Using a Surrogate Molecule: A Potential Therapeutic Agent for B Cell Malignancies

Meric A. Ovacik, A. Kamath, S. Sukumaran, 2022, Pharmaceutics.

Non-human primates in the PKPD evaluation of biologics: Needs and options to reduce, refine, and replace. A BioSafe White Paper

A. Kamath, Cheng-Pang Hsu, Hongbin Yu, 2022, mAbs.

Hyaluronic Acid-Antibody Fragment Bioconjugates for Extended Ocular Pharmacokinetics.

A. Kamath, Joyce Chan, L. Comps-Agrar, 2019, Bioconjugate chemistry.

Nonclinical Pharmacokinetics, Pharmacodynamics, and Translational Model of RO7297089, A Novel Anti-BCMA/CD16A Bispecific Tetravalent Antibody for the Treatment of Multiple Myeloma

Meric A. Ovacik, A. Kamath, A. Adedeji, 2022, The AAPS Journal.

Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily.

J. Fargnoli, J. Tokarski, G. Trainor, 2009, Journal of medicinal chemistry.

Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities.

J. Fargnoli, J. Tokarski, D. Xie, 2008, Journal of medicinal chemistry.

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.

Punit Marathe, John S Tokarski, J. Tokarski, 2004, Journal of medicinal chemistry.

A Phase 1, Randomized, Single-Ascending-Dose Study To Investigate the Safety, Tolerability, and Pharmacokinetics of DSTA4637S, an Anti-Staphylococcus aureus Thiomab Antibody-Antibiotic Conjugate, in Healthy Volunteers

N. Lewin-Koh, M. Rothenberg, A. Kamath, 2019, Antimicrobial Agents and Chemotherapy.

Preclinical discovery of ixabepilone, a highly active antineoplastic agent

F. Lee, A. Kamath, C. Fairchild, 2008, Cancer Chemotherapy and Pharmacology.

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.

J. Fargnoli, G. Derbin, J. Barrish, 2006, Journal of medicinal chemistry.

Modulation of tight junctions does not predict oral absorption of hydrophilic compounds: Use of caco-2 and calu-3 cells

S. Chong, A. Marino, R. Morrison, 2007, Archives of pharmacal research.

Complex formation of anti‐VEGF‐C with VEGF‐C released during blood coagulation resulted in an artifact in its serum pharmacokinetics

G. Fuh, A. Kamath, Y. Meng, 2020, Pharmacology research & perspectives.

Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL

F. Lee, A. Kamath, P. Marathe, 2008, Cancer Chemotherapy and Pharmacology.

Inhibitors of P-glycoprotein-mediated daunomycin transport in rat liver canalicular membrane vesicles.

M. Morris, A. Kamath, Y. Kwon, 1996, Journal of pharmaceutical sciences.

Preclinical pharmacokinetics and in vitro metabolism of brivanib (BMS-540215), a potent VEGFR2 inhibitor and its alanine ester prodrug brivanib alaninate

J. Fargnoli, A. Kamath, P. Marathe, 2009, Cancer Chemotherapy and Pharmacology.

Preclinical pharmacokinetics and oral bioavailability of BMS-310705, a novel epothilone B analog

F. Lee, A. Kamath, P. Marathe, 2005, Cancer Chemotherapy and Pharmacology.

Effect of Organic Isothiocyanates on the P-Glycoprotein- and MRP1-Mediated Transport of Daunomycin and Vinblastine

M. Morris, A. Kamath, E. Tseng, 2002, Pharmaceutical Research.

Preclinical pharmacokinetics of MFGR1877A, a human monoclonal antibody to FGFR3, and prediction of its efficacious clinical dose for the treatment of t(4;14)-positive multiple myeloma

A. Kamath, J. Qing, J. Stephan, 2012, Cancer Chemotherapy and Pharmacology.

Multiple pathways are involved in the oral absorption of BMS-262084, a tryptase inhibitor, in rats: role of paracellular transport, binding to trypsin, and P-glycoprotein efflux.

S. Chong, A. Marino, R. Morrison, 2005, Journal of pharmaceutical sciences.

P-glycoprotein plays a role in the oral absorption of BMS-387032, a potent cyclin-dependent kinase 2 inhibitor, in rats

S. Chong, A. Kamath, P. Marathe, 2005, Cancer Chemotherapy and Pharmacology.

Functional expression of P-glycoprotein in the hepatic canalicular membrane of developing rats.

M. Morris, A. Kamath, 1998, Journal of pharmaceutical sciences.

Translational pharmacokinetics and pharmacodynamics of monoclonal antibodies.

A. Kamath, Amrita V Kamath, 2016, Drug discovery today. Technologies.

Attachment Site Cysteine Thiol pKa Is a Key Driver for Site-Dependent Stability of THIOMAB Antibody-Drug Conjugates.

G. A. Lazar, Genee Y. Lee, B. Vollmar, 2017, Bioconjugate chemistry.

Discovery of Peptidomimetic Antibody-Drug Conjugate Linkers with Enhanced Protease Specificity.

S. Steinbacher, BinQing Wei, C. Eigenbrot, 2017, Journal of medicinal chemistry.

Prediction of Human Pharmacokinetics of Antibody–Drug Conjugates From Nonclinical Data

S. Girish, A. Kamath, S. Prabhu, 2019, Clinical and translational science.

Preclinical pharmacokinetics and pharmacodynamics of DCLL9718A: An antibody-drug conjugate for the treatment of acute myeloid leukemia

A. Kamath, Victor Yip, Jintang He, 2018, mAbs.

Valency of HER2 Targeting Antibodies Influences Tumor Cell Internalization and Penetration

A. Kamath, G. Ferl, M. Go, 2021, Molecular Cancer Therapeutics.

Targeting oxidized LDL improves insulin sensitivity and immune cell function in obese Rhesus macaques.

N. van Bruggen, Xia Li, A. Kamath, 2013, Molecular metabolism.

Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.

A. Doweyko, S. Spergel, R. Moquin, 2006, Bioorganic & medicinal chemistry letters.

Nonclinical toxicology development of a novel antibody antibiotic conjugate for treating invasive Staphylococcus Aureus infections

A. Kamath, W. Halpern, P. Katavolos, 2021, Toxicology and Applied Pharmacology.

Identification and characterization of an octameric PEG-protein conjugate system for intravitreal long-acting delivery to the back of the eye

P. Hass, W. Sandoval, R. Kelley, 2019, PloS one.

Influence of Charge, Hydrophobicity, and Size on Vitreous Pharmacokinetics of Large Molecules

Saileta Prabhu, R. Kelley, A. Kamath, 2019, Translational vision science & technology.

Preclinical Pharmacokinetic Considerations for the Development of Antibody Drug Conjugates

A. Kamath, S. Iyer, 2014, Pharmaceutical Research.

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.

J. Fargnoli, G. Derbin, J. Barrish, 2006, Journal of medicinal chemistry.

Characterization of Tissue Distribution, Catabolism, and Elimination of an Anti–Staphylococcus aureus THIOMAB Antibody-Antibiotic Conjugate in Rats

A. Kamath, Victor Yip, Shuguang Ma, 2020, Drug Metabolism and Disposition.

Choline uptake in human intestinal Caco-2 cells is carrier-mediated.

M. Morris, A. Kamath, I. Darling, 2003, The Journal of nutrition.

J. Fargnoli, J. Tokarski, G. Trainor, 2009, Journal of medicinal chemistry.

J. Fargnoli, G. Derbin, J. Barrish, 2008, Bioorganic & medicinal chemistry letters.

Synthesis, SAR, and Evaluation of 4-[2,4-Difluoro-5-(cyclopropylcarbamoyl)phenylamino]pyrrolo[2,1-f][1,2,4]triazine-based VEGFR-2 kinase inhibitors.

J. Fargnoli, J. Tokarski, J. Hunt, 2008, Bioorganic & medicinal chemistry letters.

Y. Shu, L. Qian, A. Kamath, 2008, Drug Metabolism and Disposition.

Utilizing PK and PD Biomarkers to Guide the First-in-Human Starting Dose Selection of MTBT1466A: A Novel Humanized Monoclonal Anti-TGFβ3 Antibody for the Treatment of Fibrotic Diseases.

Y. Wu, A. Kamath, A. M. Ovacik, 2023, Journal of pharmaceutical sciences.

A. Kamath, Summer Park, M. Maia, 2016, mAbs.

Anti–Lymphocyte Antigen 6 Complex, Locus E-Seco-Cyclopropabenzindol-4-One-Dimer Antibody-Drug Conjugate That Forms Adduct with α1-Microglobulin Demonstrates Slower Systemic Antibody Clearance and Reduced Tumor Distribution in Animals

A. Kamath, Victor Yip, Carl Ng, 2020, Drug Metabolism and Disposition.