臨床試験番号 NCT03600883 研究名 "A Phase 1/2, Study Evaluating the Safety, Tolerability, PK, and Efficacy of AMG 510 in Subjects With Solid Tumors With a Specific KRAS Mutation." - ClinicalTrials.gov
Singh J, Petter RC, Baillie TA, Whitty A (April 2011). “The resurgence of covalent drugs”. Nature Reviews. Drug Discovery10 (4): 307–317. doi:10.1038/nrd3410. PMID21455239.
Potashman MH, Duggan ME (March 2009). “Covalent modifiers: an orthogonal approach to drug design”. Journal of Medicinal Chemistry52 (5): 1231–1246. doi:10.1021/jm8008597. PMID19203292.
Liebler DC, Guengerich FP (May 2005). “Elucidating mechanisms of drug-induced toxicity”. Nature Reviews. Drug Discovery4 (5): 410–420. doi:10.1038/nrd1720. PMID15864270.
Park BK, Boobis A, Clarke S, Goldring CE, Jones D, Kenna JG, Lambert C, Laverty HG, Naisbitt DJ, Nelson S, Nicoll-Griffith DA, Obach RS, Routledge P, Smith DA, Tweedie DJ, Vermeulen N, Williams DP, Wilson ID, Baillie TA (April 2011). “Managing the challenge of chemically reactive metabolites in drug development”. Nature Reviews. Drug Discovery10 (4): 292–306. doi:10.1038/nrd3408. PMID21455238.
Singh J, Petter RC, Kluge AF (August 2010). “Targeted covalent drugs of the kinase family”. Current Opinion in Chemical Biology14 (4): 475–480. doi:10.1016/j.cbpa.2010.06.168. PMID20609616.
Singh J, Dobrusin EM, Fry DW, Haske T, Whitty A, McNamara DJ (March 1997). “Structure-based design of a potent, selective, and irreversible inhibitor of the catalytic domain of the erbB receptor subfamily of protein tyrosine kinases”. Journal of Medicinal Chemistry40 (7): 1130–1135. doi:10.1021/jm960380s. PMID9089334.
Hagel M, Niu D, St Martin T, Sheets MP, Qiao L, Bernard H, Karp RM, Zhu Z, Labenski MT, Chaturvedi P, Nacht M, Westlin WF, Petter RC, Singh J (January 2011). “Selective irreversible inhibition of a protease by targeting a noncatalytic cysteine”. Nature Chemical Biology7 (1): 22–24. doi:10.1038/nchembio.492. PMID21113170.
Srinivasan B (March 2021). “Explicit Treatment of Non-Michaelis-Menten and Atypical Kinetics in Early Drug Discovery*”. ChemMedChem16 (6): 899–918. doi:10.1002/cmdc.202000791. PMID33231926.
Garrido-Charles A, Huet A, Matera C, Thirumalai A, Hernando J, Llebaria A, Moser T, Gorostiza P (June 2022). “Fast Photoswitchable Molecular Prosthetics Control Neuronal Activity in the Cochlea”. Journal of the American Chemical Society144 (21): 9229–9239. doi:10.1101/2021.05.25.445123. PMID35584208.
Bauer RA (September 2015). “Covalent inhibitors in drug discovery: from accidental discoveries to avoided liabilities and designed therapies”. Drug Discovery Today20 (9): 1061–1073. doi:10.1016/j.drudis.2015.05.005. PMID26002380.
Nakayama S, Atsumi R, Takakusa H, Kobayashi Y, Kurihara A, Nagai Y, Nakai D, Okazaki O (September 2009). “A zone classification system for risk assessment of idiosyncratic drug toxicity using daily dose and covalent binding”. Drug Metabolism and Disposition37 (9): 1970–1977. doi:10.1124/dmd.109.027797. PMID19487250.
Singh J, Petter RC, Baillie TA, Whitty A (April 2011). “The resurgence of covalent drugs”. Nature Reviews. Drug Discovery10 (4): 307–317. doi:10.1038/nrd3410. PMID21455239.
Potashman MH, Duggan ME (March 2009). “Covalent modifiers: an orthogonal approach to drug design”. Journal of Medicinal Chemistry52 (5): 1231–1246. doi:10.1021/jm8008597. PMID19203292.
Liebler DC, Guengerich FP (May 2005). “Elucidating mechanisms of drug-induced toxicity”. Nature Reviews. Drug Discovery4 (5): 410–420. doi:10.1038/nrd1720. PMID15864270.
Park BK, Boobis A, Clarke S, Goldring CE, Jones D, Kenna JG, Lambert C, Laverty HG, Naisbitt DJ, Nelson S, Nicoll-Griffith DA, Obach RS, Routledge P, Smith DA, Tweedie DJ, Vermeulen N, Williams DP, Wilson ID, Baillie TA (April 2011). “Managing the challenge of chemically reactive metabolites in drug development”. Nature Reviews. Drug Discovery10 (4): 292–306. doi:10.1038/nrd3408. PMID21455238.
Singh J, Petter RC, Kluge AF (August 2010). “Targeted covalent drugs of the kinase family”. Current Opinion in Chemical Biology14 (4): 475–480. doi:10.1016/j.cbpa.2010.06.168. PMID20609616.
Singh J, Dobrusin EM, Fry DW, Haske T, Whitty A, McNamara DJ (March 1997). “Structure-based design of a potent, selective, and irreversible inhibitor of the catalytic domain of the erbB receptor subfamily of protein tyrosine kinases”. Journal of Medicinal Chemistry40 (7): 1130–1135. doi:10.1021/jm960380s. PMID9089334.
Hagel M, Niu D, St Martin T, Sheets MP, Qiao L, Bernard H, Karp RM, Zhu Z, Labenski MT, Chaturvedi P, Nacht M, Westlin WF, Petter RC, Singh J (January 2011). “Selective irreversible inhibition of a protease by targeting a noncatalytic cysteine”. Nature Chemical Biology7 (1): 22–24. doi:10.1038/nchembio.492. PMID21113170.
Srinivasan B (March 2021). “Explicit Treatment of Non-Michaelis-Menten and Atypical Kinetics in Early Drug Discovery*”. ChemMedChem16 (6): 899–918. doi:10.1002/cmdc.202000791. PMID33231926.
Garrido-Charles A, Huet A, Matera C, Thirumalai A, Hernando J, Llebaria A, Moser T, Gorostiza P (June 2022). “Fast Photoswitchable Molecular Prosthetics Control Neuronal Activity in the Cochlea”. Journal of the American Chemical Society144 (21): 9229–9239. doi:10.1101/2021.05.25.445123. PMID35584208.
Bauer RA (September 2015). “Covalent inhibitors in drug discovery: from accidental discoveries to avoided liabilities and designed therapies”. Drug Discovery Today20 (9): 1061–1073. doi:10.1016/j.drudis.2015.05.005. PMID26002380.
Nakayama S, Atsumi R, Takakusa H, Kobayashi Y, Kurihara A, Nagai Y, Nakai D, Okazaki O (September 2009). “A zone classification system for risk assessment of idiosyncratic drug toxicity using daily dose and covalent binding”. Drug Metabolism and Disposition37 (9): 1970–1977. doi:10.1124/dmd.109.027797. PMID19487250.
臨床試験番号 NCT03600883 研究名 "A Phase 1/2, Study Evaluating the Safety, Tolerability, PK, and Efficacy of AMG 510 in Subjects With Solid Tumors With a Specific KRAS Mutation." - ClinicalTrials.gov