Lorlatinib effective in multiple settings.
Sidaway P.
Nat Rev Clin Oncol · journal article · DOI 10.1038/s41571-018-0141-9 PUBLICATION REGISTRY
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13 hitsLorlatinib for the treatment of patients with non-small cell lung cancer.
Akamine T, Toyokawa G, Tagawa T, Yamazaki K, Seto T, Takeo S, Mori M.
Drugs Today (Barc) · journal article · DOI 10.1358/dot.2019.55.2.2927983Lorlatinib: First Global Approval.
Syed YY.
Drugs · review; journal article · DOI 10.1007/s40265-018-1041-0Lorlatinib in patients with ALK-positive non-small-cell lung cancer: results from a global phase 2 study.
Solomon BJ, Besse B, Bauer TM, Felip E, Soo RA, Camidge DR, Chiari R, Bearz A, Lin CC, Gadgeel SM, Riely GJ, Tan EH, Seto T, James LP, Clancy JS, Abbattista A, Martini JF, Chen J, Peltz G, Thurm H, Ou SI, Shaw AT.
Lancet Oncol · clinical trial, phase ii; research support, non-u.s. gov't; multicenter study; journal article · DOI 10.1016/s1470-2045(18)30649-1P-glycoprotein (MDR1/ABCB1) restricts brain accumulation and cytochrome P450-3A (CYP3A) limits oral availability of the novel ALK/ROS1 inhibitor lorlatinib.
Li W, Sparidans RW, Wang Y, Lebre MC, Wagenaar E, Beijnen JH, Schinkel AH.
Int J Cancer · research support, non-u.s. gov't; journal article · DOI 10.1002/ijc.31582Synthesis and preliminary PET imaging of <sup>11</sup>C and <sup>18</sup>F isotopologues of the ROS1/ALK inhibitor lorlatinib.
Collier TL, Normandin MD, Stephenson NA, Livni E, Liang SH, Wooten DW, Esfahani SA, Stabin MG, Mahmood U, Chen J, Wang W, Maresca K, Waterhouse RN, El Fakhri G, Richardson P, Vasdev N.
Nat Commun · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1038/ncomms15761Tackling ALK in non-small cell lung cancer: the role of novel inhibitors.
Facchinetti F, Tiseo M, Di Maio M, Graziano P, Bria E, Rossi G, Rossi G, Novello S.
Transl Lung Cancer Res · review-article; review; journal article · DOI 10.21037/tlcr.2016.06.10Conformational Studies and Atropisomerism Kinetics of the ALK Clinical Candidate Lorlatinib (PF-06463922) and Desmethyl Congeners.
Elleraas J, Ewanicki J, Johnson TW, Sach NW, Collins MR, Richardson PF.
Angew Chem Int Ed Engl · journal article · DOI 10.1002/anie.201509240Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F.
Shaw AT, Friboulet L, Leshchiner I, Gainor JF, Bergqvist S, Brooun A, Burke BJ, Deng YL, Liu W, Dardaei L, Frias RL, Schultz KR, Logan J, James LP, Smeal T, Timofeevski S, Katayama R, Iafrate AJ, Le L, McTigue M, Getz G, Johnson TW, Engelman JA.
N Engl J Med · research support, non-u.s. gov't; research-article; clinical trial, phase i; journal article; case reports; research support, n.i.h., extramural · DOI 10.1056/nejmoa1508887PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations.
Zou HY, Li Q, Engstrom LD, West M, Appleman V, Wong KA, McTigue M, Deng YL, Liu W, Brooun A, Timofeevski S, McDonnell SR, Jiang P, Falk MD, Lappin PB, Affolter T, Nichols T, Hu W, Lam J, Johnson TW, Smeal T, Charest A, Fantin VR.
Proc Natl Acad Sci U S A · research-article; journal article · DOI 10.1073/pnas.1420785112Mechanistic understanding of translational pharmacokinetic-pharmacodynamic relationships in nonclinical tumor models: a case study of orally available novel inhibitors of anaplastic lymphoma kinase.
Yamazaki S, Lam JL, Zou HY, Wang H, Smeal T, Vicini P.
Drug Metab Dispos · journal article · DOI 10.1124/dmd.114.061143Translational pharmacokinetic-pharmacodynamic modeling for an orally available novel inhibitor of anaplastic lymphoma kinase and c-Ros oncogene 1.
Yamazaki S, Lam JL, Zou HY, Wang H, Smeal T, Vicini P.
J Pharmacol Exp Ther · journal article · DOI 10.1124/jpet.114.217141Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.
Johnson TW, Richardson PF, Bailey S, Brooun A, Burke BJ, Collins MR, Cui JJ, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Huang Q, Kania RS, Kath JC, Lam H, Lam JL, Le PT, Lingardo L, Liu W, McTigue M, Palmer CL, Sach NW, Smeal T, Smith GL, Stewart AE, Timofeevski S, Zhu H, Zhu J, Zou HY, Edwards MP.
J Med Chem · journal article · DOI 10.1021/jm500261q