Selpercatinib for lung and thyroid cancers with RET gene mutations or fusions

被引:4
作者
Zheng, H. [1 ]
Chen, Z-S [2 ]
Li, J. [1 ]
机构
[1] China Med Univ, Affiliated Hosp 1, Shenyang 110001, Peoples R China
[2] St Johns Univ, Coll Pharm & Hlth Sci, Dept Pharmaceut Sci, New York, NY 11439 USA
关键词
Selpercatinib; Rearranged during transfection (RET) gene mutations or fusions; Tyrosine kinase inhibitors; Antitumor drugs; Thyroid cancer; Lung cancer; Targeted therapy; Solid tumors therapy; OPEN-LABEL; ACQUIRED-RESISTANCE; CABOZANTINIB; PRALSETINIB; VANDETANIB; EFFICACY; PHASE-2; TRIAL;
D O I
10.1358/dot.2021.57.10.3313852
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Aberrations in oncogene RET (rearranged during transfection) have been found to be the cause of different kinds of malignancies, especially in lung and thyroid cancers. Targeted therapy of RET-altered cancers using multi-kinase inhibitors (MKIs) has demonstrated limited clinical efficacy due to off-target toxicity. In May 2020, the U.S. Food and Drug Administration (FDA) approved a novel specific RET inhibitor for use in some subtypes of lung and thyroid cancers with RET alterations. In this review, we summarize the mechanism of action, pharmaceutical properties and clinical data of selpercatinib, and share some of our perspectives.
引用
收藏
页码:621 / 629
页数:9
相关论文
共 46 条
  • [1] Systemic and CNS Activity of Selective RET Inhibition With Selpercatinib (LOXO-292) in a Patient With RET-Mutant Medullary Thyroid Cancer With Extensive CNS Metastases
    Andreev-Drakhlin, Alexander
    Cabanillas, Maria
    Amini, Behrang
    Subbiah, Vivek
    [J]. JCO PRECISION ONCOLOGY, 2020, 4 : 1302 - 1306
  • [2] Brandhuber B., 2016, 28 EORTC NCI AACR S
  • [3] Management of treatment-related toxicities in advanced medullary thyroid cancer
    Brose, Marcia S.
    Bible, Keith C.
    Chow, Laura Q. M.
    Gilbert, Jill
    Grande, Carolyn
    Worden, Francis
    Haddad, Robert
    [J]. CANCER TREATMENT REVIEWS, 2018, 66 : 64 - 73
  • [4] Genetic Landscape of Somatic Mutations in a Large Cohort of Sporadic Medullary Thyroid Carcinomas Studied by Next-Generation Targeted Sequencing
    Ciampi, Raffaele
    Romei, Cristina
    Ramone, Teresa
    Prete, Alessandro
    Tacito, Alessia
    Cappagli, Virginia
    Bottici, Valeria
    Viola, David
    Torregrossa, Liborio
    Ugolini, Clara
    Basolo, Fulvio
    Elisei, Rossella
    [J]. ISCIENCE, 2019, 20 : 324 - +
  • [5] Rethinking treatment for RET-altered lung and thyroid cancers: selpercatinib approval by the EMA
    Della Corte, C. M.
    Morgillo, F.
    [J]. ESMO OPEN, 2021, 6 (01)
  • [6] Response to RET-Specific Therapy in RET Fusion-Positive Anaplastic Thyroid Carcinoma
    Dias-Santagata, Dora
    Lennerz, Jochen K.
    Sadow, Peter M.
    Frazier, Ryan P.
    Raju, Sandya Govinda
    Henry, Dahlia
    Chung, Trisha
    Kherani, Jennifer
    Rothenberg, S. Michael
    Wirth, Lori J.
    [J]. THYROID, 2020, 30 (09) : 1384 - 1389
  • [7] Efficacy of Selpercatinib in RET Fusion-Positive Non-Small-Cell Lung Cancer
    Drilon, A.
    Oxnard, G. R.
    Tan, D. S. W.
    Loong, H. H. F.
    Johnson, M.
    Gainor, J.
    McCoach, C. E.
    Gautschi, O.
    Besse, B.
    Cho, B. C.
    Peled, N.
    Weiss, J.
    Kim, Y. -J.
    Ohe, Y.
    Nishio, M.
    Park, K.
    Patel, J.
    Seto, T.
    Sakamoto, T.
    Rosen, E.
    Shah, M. H.
    Barlesi, F.
    Cassier, P. A.
    Bazhenova, L.
    De Braud, F.
    Garralda, E.
    Velcheti, V.
    Satouchi, M.
    Ohashi, K.
    Pennell, N. A.
    Reckamp, K. L.
    Dy, G. K.
    Wolf, J.
    Solomon, B.
    Falchook, G.
    Ebata, K.
    Nguyen, M.
    Nair, B.
    Zhu, E. Y.
    Yang, L.
    Huang, X.
    Olek, E.
    Rothenberg, S. M.
    Goto, K.
    Subbiah, V.
    [J]. NEW ENGLAND JOURNAL OF MEDICINE, 2020, 383 (09) : 813 - 824
  • [8] Frequency of Brain Metastases and Multikinase Inhibitor Outcomes in Patients With RET-Rearranged Lung Cancers
    Drilon, Alexander
    Lin, Jessica J.
    Filleron, Thomas
    Ni, Ai
    Milia, Julie
    Bergagnini, Isabella
    Hatzoglou, Vaios
    Velcheti, Vamsidhar
    Offin, Michael
    Li, Bob
    Carbone, David P.
    Besse, Benjamin
    Mok, Tony
    Awad, Mark M.
    Wolf, Jurgen
    Owen, Dwight
    Camidge, D. Ross
    Riely, Gregory J.
    Peled, Nir
    Kris, Mark G.
    Mazieres, Julien
    Gainor, Justin F.
    Gautschi, Oliver
    [J]. JOURNAL OF THORACIC ONCOLOGY, 2018, 13 (10) : 1595 - 1601
  • [9] Drilon A, 2018, NAT REV CLIN ONCOL, V15, P151, DOI [10.1038/nrclinonc.2017.175, 10.1038/nrclinonc.2017.188]
  • [10] Cabozantinib in patients with advanced RET-rearranged non-small-cell lung cancer: an open-label, single-centre, phase 2, single-arm trial
    Drilon, Alexander
    Rekhtman, Natasha
    Arcila, Maria
    Wang, Lu
    Ni, Andy
    Albano, Melanie
    Van Voorthuysen, Martine
    Somwar, Romel
    Smith, Roger S.
    Montecalvo, Joseph
    Plodkowski, Andrew
    Ginsberg, Michelle S.
    Riely, Gregory J.
    Rudin, Charles M.
    Ladanyi, Marc
    Kris, Mark G.
    [J]. LANCET ONCOLOGY, 2016, 17 (12) : 1653 - 1660