Brigimadlin
Appearance
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Names | |
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IUPAC name
(3S,10'S,11'S,14'S)-6-chloro-11'-(3-chloro-2-fluorophenyl)-13'-(cyclopropylmethyl)-6'-methyl-2-oxospiro[1H-indole-3,12'-8,9,13-triazatetracyclo[7.6.0.02,7.010,14]pentadeca-1,3,5,7-tetraene]-5'-carboxylic acid
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Identifiers | |
3D model (JSmol)
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EC Number |
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KEGG | |
PubChem CID
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UNII | |
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Properties | |
C31H25Cl2FN4O3 | |
Molar mass | 591.46 g·mol−1 |
Hazards | |
GHS labelling:[1] | |
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Danger | |
H300, H360Df, H372, H413 | |
P203, P260, P264, P270, P273, P280, P301+P316, P318, P319, P321, P330, P405, P501 | |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Brigimadlin (BI-907828) is a small molecule MDM2-TP53 inhibitor developed for liposarcoma.[2][3][4][5][6]
References
[edit]- ^ "Brigimadlin". pubchem.ncbi.nlm.nih.gov.
- ^ Rinnenthal, Joerg; Rudolph, Dorothea; Blake, Sophia; Gollner, Andreas; Wernitznig, Andreas; Weyer-Czernilofsky, Ulrike; Haslinger, Christian; Garin-Chesa, Pilar; Moll, Jürgen; Kraut, Norbert; McConnell, Darryl; Quant, Jens (1 July 2018). "Abstract 4865: BI 907828: A highly potent MDM2 inhibitor with low human dose estimation, designed for high-dose intermittent schedules in the clinic". Cancer Research. 78 (13_Supplement): 4865. doi:10.1158/1538-7445.AM2018-4865. S2CID 56768874.
- ^ Rudolph, Dorothea; Reschke, Markus; Blake, Sophia; Rinnenthal, Jörg; Wernitznig, Andreas; Weyer-Czernilofsky, Ulrike; Gollner, Andreas; Haslinger, Christian; Garin-Chesa, Pilar; Quant, Jens; McConnell, Darryl B.; Norbert, Kraut; Moll, Jürgen (1 July 2018). "Abstract 4866: BI 907828: A novel, potent MDM2 inhibitor that induces antitumor immunologic memory and acts synergistically with an anti-PD-1 antibody in syngeneic mouse models of cancer". Cancer Research. 78 (13_Supplement): 4866. doi:10.1158/1538-7445.AM2018-4866. S2CID 80770832.
- ^ Cornillie, J.; Wozniak, A.; Li, H.; Gebreyohannes, Y. K.; Wellens, J.; Hompes, D.; Debiec-Rychter, M.; Sciot, R.; Schöffski, P. (April 2020). "Anti-tumor activity of the MDM2-TP53 inhibitor BI-907828 in dedifferentiated liposarcoma patient-derived xenograft models harboring MDM2 amplification". Clinical and Translational Oncology. 22 (4): 546–554. doi:10.1007/s12094-019-02158-z. PMID 31201607. S2CID 189862528.
- ^ Schöffski, Patrick; Lahmar, Mehdi; Lucarelli, Anthony; Maki, Robert G (March 2023). "Brightline-1: phase II/III trial of the MDM2–p53 antagonist BI 907828 versus doxorubicin in patients with advanced DDLPS". Future Oncology. 19 (9): 621–629. doi:10.2217/fon-2022-1291. PMID 36987836. S2CID 257802972.
- ^ Schoeffski, P.; Lorusso, P.; Yamamoto, N.; Lugowska, I.; Moreno Garcia, V.; Lauer, U.; Hu, C.; Jayadeva, G.; Lahmar, M.; Gounder, M. (October 2023). "673P A phase I dose-escalation and expansion study evaluating the safety and efficacy of the MDM2–p53 antagonist brigimadlin (BI 907828) in patients (pts) with solid tumours". Annals of Oncology. 34: S472–S473. doi:10.1016/j.annonc.2023.09.1859. S2CID 264392338.