Birinapant

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Birinapant is a clinical SMAC mimetic (enhances apoptosis) undergoing development to treat multiple malignancies including ovarian cancer[1], lymphoma[2], acute myeloid leukaemia, in combination with emricasan[3], acute lymphoblastic leukaemia[4], and colorectal tumours[5].

References

  1. Noonan AM, Bunch KP, Chen JQ, Herrmann MA, Lee JM, Kohn EC, O'Sullivan CC, Jordan E, Houston N, Takebe N, Kinders RJ, Cao L, Peer CJ, Figg WD, Annunziata CM. Pharmacodynamic markers and clinical results from the phase 2 study of the SMAC mimetic birinapant in women with relapsed platinum-resistant or -refractory epithelial ovarian cancer. Cancer. 2016 Feb 15; 122(4):588-97.(Link to article – subscription may be required.)
  2. Amaravadi RK, Schilder RJ, Martin LP, Levin M, Graham MA, Weng DE, Adjei AA. A Phase I Study of the SMAC-Mimetic Birinapant in Adults with Refractory Solid Tumors or Lymphoma. Molecular cancer therapeutics. 2015 Nov; 14(11):2569-75.(Link to article – subscription may be required.)
  3. Brumatti G, Ma C, Lalaoui N, Nguyen NY, Navarro M, Tanzer MC, Richmond J, Ghisi M, Salmon JM, Silke N, Pomilio G, Glaser SP, de Valle E, Gugasyan R, Gurthridge MA, Condon SM, Johnstone RW, Lock R, Salvesen G, Wei A, Vaux DL, Ekert PG, Silke J. The caspase-8 inhibitor emricasan combines with the SMAC mimetic birinapant to induce necroptosis and treat acute myeloid leukemia. Science translational medicine. 2016 May 18; 8(339):339ra69.(Link to article – subscription may be required.)
  4. Richmond J, Robbins A, Evans K, Beck D, Kurmasheva RT, Billups CA, Carol H, Heatley S, Sutton R, Marshall GM, White D, Pimanda J, Houghton PJ, Smith MA, Lock RB. Acute Sensitivity of Ph-like Acute Lymphoblastic Leukemia to the SMAC-Mimetic Birinapant. Cancer research. 2016 Aug 1; 76(15):4579-91.(Link to article – subscription may be required.)
  5. Perimenis P, Galaris A, Voulgari A, Prassa M, Pintzas A. IAP antagonists Birinapant and AT-406 efficiently synergise with either TRAIL, BRAF, or BCL-2 inhibitors to sensitise BRAFV600E colorectal tumour cells to apoptosis. BMC cancer. 2016; 16:624.(Epub) (Link to article – subscription may be required.)
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