Deruxtecan Explained

Deruxtecan is a chemical compound and a derivative of exatecan that acts as topoisomerase I inhibitor.[1]

It is available linked to specific monoclonal antibody (antibody–drug conjugate), such as:

Notes and References

  1. Web site: A HER2-Targeting Antibody–Drug Conjugate, Trastuzumab Deruxtecan (DS-8201a), Enhances Antitumor Immunity in a Mouse Model . 23 December 2019 . 24 September 2020 . https://web.archive.org/web/20200924062005/https://mct.aacrjournals.org/content/molcanther/17/7/1494.full.pdf . live .
  2. FDA approves new treatment option for patients with HER2-positive breast cancer who have progressed on available therapies . U.S.Food and Drug Administration (FDA) . 20 December 2019 . https://web.archive.org/web/20191220192916/https://www.fda.gov/news-events/press-announcements/fda-approves-new-treatment-option-patients-her2-positive-breast-cancer-who-have-progressed-available . 20 December 2019 . live . 20 December 2019.
  3. Yu . H.A. . Baik . C.S. . Gold . K. . Hayashi . H. . Johnson . M. . Koczywas . M. . Murakami . H. . Nishio . M. . Steuer . C. . Su . W-C. . Yang . J. . Karam . S. . Qi . Z. . Qiu . Y. . Chen . S. . Yu . C. . Jänne . P.A. . LBA62 Efficacy and safety of patritumab deruxtecan (U3-1402), a novel HER3 directed antibody drug conjugate, in patients (pts) with EGFR-mutated (EGFRm) NSCLC . Annals of Oncology . September 2020 . 31 . S1189–S1190 . 10.1016/j.annonc.2020.08.2295. 225184933 . free .
  4. Krop . Ian E. . Masuda . Norikazu . Mukohara . Toru . Takahashi . Shunji . Nakayama . Takahiro . Inoue . Kenichi . Iwata . Hiroji . Toyama . Tatsuya . Yamamoto . Yutaka . Hansra . Damien Mikael . Takahashi . Masato . Osaki . Akihiko . Koyama . Kumiko . Inoue . Tatsuya . Yonekura . Takatoshi . Mostillo . Joseph . Ohwada . Shoichi . Tanaka . Yoshimi . Sternberg . David W. . Yonemori . Kan . Results from the phase 1/2 study of patritumab deruxtecan, a HER3-directed antibody-drug conjugate (ADC), in patients with HER3-expressing metastatic breast cancer (MBC). . Journal of Clinical Oncology . 1 June 2022 . 40 . 16_suppl . 1002 . 10.1200/JCO.2022.40.16_suppl.1002. 249454563 .
  5. Jänne . Pasi A. . Baik . Christina . Su . Wu-Chou . Johnson . Melissa L. . Hayashi . Hidetoshi . Nishio . Makoto . Kim . Dong-Wan . Koczywas . Marianna . Gold . Kathryn A. . Steuer . Conor E. . Murakami . Haruyasu . Yang . James Chih-Hsin . Kim . Sang-We . Vigliotti . Michele . Shi . Rong . Qi . Zhenhao . Qiu . Yang . Zhao . Lihui . Sternberg . David . Yu . Channing . Yu . Helena A. . Efficacy and Safety of Patritumab Deruxtecan (HER3-DXd) in EGFR Inhibitor–Resistant, EGFR -Mutated Non–Small Cell Lung Cancer . Cancer Discovery . 1 January 2022 . 12 . 1 . 74–89 . 10.1158/2159-8290.CD-21-0715. 34548309 . 9401524 .
  6. Katsumata . Len . Deguchi . Tsuneo . Hasegawa . Jun . Yamato . Michiko . Nishiya . Yumi . Watanabe . Akiko . Honda . Tomoyo . Minami . Megumi . Kasanuki . Naomi . Maejima . Takanori . Muramatsu . Sumie . Herrmann . Monika . Schulte . Nina . Polier . Gernot . Wang . Xuya . Yoshida . Takanori . Izumi . Nanae . Qian . Xiaozhong . Agatsuma . Toshinori . Nakamaru . Kenji . Abstract 4891: Ifinatamab deruxtecan (I-DXd), a novel B7-H3-targeting antibody-drug conjugate, demonstrates efficient payload delivery into tumor through target-dependent internalization . Cancer Research . 4 April 2023 . 83 . 7_Supplement . 4891 . 10.1158/1538-7445.AM2023-4891. 259620618 .
  7. Patel . M.R. . Doi . T. . Koyama . T. . Falchook . G.S. . Friedman . C.F. . Piha-Paul . S.A. . Gutierrez . M. . Awad . M.M. . Mattour . A.H. . Satoh . T. . Okamoto . N. . Singh . J. . Yoshizuka . N. . Qian . M. . Qian . X. . Tran . B.P. . Dosunmu . O. . Lu . P. . Johnson . M.L. . 690P Ifinatamab deruxtecan (I-DXd; DS-7300) in patients with advanced solid tumors: Updated clinical and biomarker results from a phase I/II study . Annals of Oncology . October 2023 . 34 . S481–S482 . 10.1016/j.annonc.2023.09.1876. 264385889 .