Medicinal Chemistry Reviews

Volume 52, Chapter 3

Discovery of the ALK/ROS1 Inhibitor, Lorlatinib (PF-06463922)

1.          Introduction                                                                                                               45

2.         Next-Generation ALK Program—Acyclic (or Non-Macrocyclic) 

            Chemical Space                                                                                                         48

3.         Macrocyclic Inhibitors—Discovery of Lorlatinib (16)                                             51

4.         Selectivity Strategy                                                                                                    54

5.         CNS Exposure                                                                                                            57

6.         Acyclics versus Macrocycles                                                                          60

7.         Overview of Lorlatinib (16)                                                                                       61

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