Page 24 - 《中国药科大学学报》2025年第5期
P. 24

556                      学报   Journal of China Pharmaceutical University 2025, 56(5): 548 − 556  第 56 卷

                    lethality[J]. Front Oncol, 2023, 13: 1264785.  [27]   Abbisko  therapeutics  co  Ltd.  Nitrogen-containing  fused  three
               [15]   Mavrakis  KJ,  Robert  McDonald  E  3rd,  Schlabach  MR,  et  al.  ring  PRMT5  inhibitor,  and  preparation  method  therefor  and
                    Disordered  methionine  metabolism  in  MTAP/CDKN2A-delet-  pharmaceutical  use  thereof:  WO2024027370A1[P].  2024-02-
                    ed  cancers  leads  to  dependence  on  PRMT5[J].  Science,  2016,  08[2025-01-28].
                    351(6278): 1208-1213.                       [28]   Tango Therapeutics Inc. Piperidin-1-yl-N-pyridin-3-yl-2-oxoac-
               [16]   Marjon  K,  Cameron  MJ,  Quang  P,  et  al.  MTAP  deletions  in  etamide derivatives useful for the treatment of MTAP-deficient
                    cancer   create   vulnerability   to   targeting   of   the  and/or  MTA-accumulating  cancers:  WO2022026892A1[P].
                    MAT2A/PRMT5/RIOK1  axis[J].  Cell  Rep,  2016,  15(3):  574-  2022-02-03[2025-01-28].
                    587.                                        [29]   Briggs KJ, Tsai A, Zhang MJ, et al. Abstract 4970: TNG462 is
               [17]   Hu  M,  Chen  X.  A  review  of  the  known  MTA-cooperative  a potential best-in-class MTA-cooperative PRMT5 inhibitor for
                    PRMT5 inhibitors[J]. RSC Adv, 2024, 14(53): 39653-39691.  the  treatment  of  MTAP-deleted  solid  tumors[J].  Cancer  Res,
               [18]   Smith  CR,  Kulyk  S,  Ahmad  MUD,  et  al.  Fragment  optimiza-  2023, 83(Suppl 7): 4970.
                    tion and elaboration strategies–the discovery of two lead series  [30]   Cottrell  KM,  Briggs  KJ,  Whittington  DA,  et  al.  Discovery  of
                    of PRMT5/MTA inhibitors from five fragment hits[J]. RSC Med  TNG908:  a  selective,  brain  penetrant,  MTA-cooperative
                    Chem, 2022, 13(12): 1549-1564.                   PRMT5 inhibitor that is synthetically lethal with MTAP-deleted
               [19]   Smith CR, Aranda R, Bobinski TP, et al. Fragment-based dis-  cancers[J]. J Med Chem, 2024, 67(8): 6064-6080.
                    covery  of  MRTX1719,  a  synthetic  lethal  inhibitor  of  the  [31]   Briggs KJ, Cottrell KM, Tonini MR, et al. TNG908 is a brain-
                    PRMT5•MTA complex for the treatment of MTAP-deleted can-  penetrant, MTA-cooperative PRMT5 inhibitor developed for the
                    cers[J]. J Med Chem, 2022, 65(3): 1749-1766.     treatment of MTAP-deleted cancers[J]. Transl Oncol, 2025, 52:
               [20]   Smith CR, Aranda R, Christensen JG, et al. Design and evalua-  102264.
                    tion  of  achiral,  non-atropisomeric  4-(aminomethyl)phthalazin-  [32]   Zhang  MJ,  Tsai  A,  Cottrell  K,  et  al.  DDDR-33.  TNG908,  a
                    1(2H)-one  derivatives  as  novel  PRMT5/MTA  inhibitors[J].  brain-penetrant  mta-cooperative PRMT5  inhibitor,  is   effica-
                    Bioorg Med Chem, 2022, 71: 116947.               cious  in  preclinical  MTAP-deleted models  including   glioblas-
               [21]   Belmontes B, Slemmons KK, Su C, et al. AMG 193, a clinical  toma[J]. Neuro-Oncology, 2023, 25(Suppl 5): v113.
                    stage MTA-cooperative PRMT5 inhibitor, drives antitumor ac-  [33]   Cottrell KM, Briggs KJ, Tsai A, et al. Discovery of TNG462: a
                    tivity  preclinically  and  in  patients  with  MTAP-deleted  highly potent and selective MTA-cooperative PRMT5 inhibitor
                    cancers[J]. Cancer Discov, 2025, 15(1): 139-161.  to  target  cancers  with  MTAP  deletion[J].  J  Med  Chem,  2025,
               [22]   Sarvary I, Vestergaard M, Moretti L, et al. From DNA-encoded  68(5): 5097-5119.
                    library screening to AM-9747: an MTA-cooperative PRMT5 in-  [34]   AstraZeneca AB. MTA-cooperative PRMT5 inhibitors for use
                    hibitor with potent oral in vivo efficacy[J]. J Med Chem, 2025,  in  the  treatment  of  cancer:  WO2024038004A1[P].  2024-02-
                    68(6): 6534-6557.                                22[2025-01-28].
               [23]   Amgen Inc. AMG 193 alone or in combination with other thera-  [35]   AstraZeneca  AB.  Spirocyclic  compounds:  WO2023036974A1
                    pies in  subjects  with  advanced  thoracic  tumors  with   homozy-  [P]. 2023-03-16[2025-01-28].
                    gous  MTAP-deletion  (master  protocol)[EB/OL].  (2025-04-  [36]   Smith JM, Barlaam B, Beattie D, et al. Discovery and in vivo
                    04)[2025-04-07]. https://clinicaltrials.gov/study/NCT06333951.  efficacy of AZ-PRMT5i-1, a novel PRMT5 inhibitor with high
               [24]   Amgen  Inc.  A  study  evaluating  AMG  193  in  combination  MTA  cooperativity[J].  J  Med  Chem,  2024,  67(16):  13604-
                    with other therapies in participants with advanced gastrointesti-  13638.
                    nal,  biliary  tract,  or  pancreatic  cancers  with  homozygous  [37]   Spira AI, Lau J, Hattersley MM, et al. PRIMROSE: a modular
                    methylthioadenosine  phosphorylase  (MTAP)-deletion[EB/OL].  phase 1/2a study of AZD3470, an MTA-cooperative PRMT5 in-
                    (2025-04-04)[2025-04-07]. https://clinicaltrials.gov/study/  hibitor,  in  patients  with  MTAP  deficient  advanced  solid
                    NCT06360354.                                     tumors[J]. J Clin Oncol, 2024, 42(Suppl 16): TPS3179.
               [25]   Amgen  Inc.  A  phase  1/2  study  of  AMG  193  in  combination  [38]   Smith  J,  Urosevic  J,  Moore  S,  et  al.  First  disclosure  of
                    with  IDE397  in  participants  with  advanced  methylthioa-  AZD3470, a highly potent MTA-cooperative PRMT5 inhibitor
                    denosine  phosphorylase  (MTAP)-null  solid  tumors[EB/OL].  in  PRIMROSE  and  PRIMAVERA  clinical  studies[J].  Eur  J
                    (2025-02-27)[2025-04-07]. https://clinicaltrials.gov/study/  Cancer, 2024, 211: 114668.
                    NCT05975073.                                [39]   Gjuka D, Adib E, Garrison K, et al. Enzyme-mediated deple-
               [26]   Shanghai apeiron therapeutics company Ltd. Novel PRMT5 in-  tion of methylthioadenosine restores T cell function in MTAP-
                    hibitor  and  use  Thereof:  WO2024032572A1[P].  2024-02-  deficient  tumors  and  reverses  immunotherapy  resistance[J].
                    15[2025-01-28].                                  Cancer Cell, 2023, 41(10): 1774-1787. e9.
   19   20   21   22   23   24   25   26   27   28   29