From: The design and development of covalent protein-protein interaction inhibitors for cancer treatment
Compound name | Therapeutic area | Highest phase reached |
---|---|---|
BCL-2 family | ||
 Obatoclax (CEP-41601, GX015-070) | Phase III (discontinued) | |
 Navitoclax (ABT-263) | Chronic lymphocytic leukemia/prostate cancer | Phase II (completed) |
 Venetoclax (ABT-199) | Leukemia/acute myeloid leukemia | Phase I |
MDM2–p53 pathway | ||
 Idasanutlin (RO5503781) | Leukemia/acute myeloid leukemia | Phase III |
 AMG232 | Metastatic melanoma | Phase I/II |
 CGM097 | Solid tumor with wild-type p53 | Phase I |
 DS-3032b | Advanced solid tumors/lymphomas | Phase I |
 ALRN-6924 | Acute myeloid leukemia /advanced myelodysplastic syndrome | Phase I |
 MK-8242 | Advanced solid tumors | Phase I |
 JNJ-26854165 | Advanced stage or refractory solid tumors | Phase I (completed) |
 RG-7112 (RO5045337) | Hematologic neoplasms | Phase I (completed) |
 SAR-405838 | Malignant neoplasms | Phase I |
IAP pathway | ||
 AT-406 (Debio-1143) | Solid tumor | Phase II |
 LCL-161 | Breast cancer | Phase II |
 Birinapant (TL32711) | Advanced or metastatic solid tumors | Phase I/II |
 ASTX-660 | Advanced solid tumors and lymphomas | Phase I/II |
 AEG40826 (HGS1029) | Advanced solid tumors | Phase I |
 CUDC-427 (GDC-0917) | Lymphoma | Phase I |
 GDC-0152 (RG-7419) | Advanced or metastatic malignancies | Phase I (discontinued) |
 GSK525762 | Breast cancer | Phase I/II |
 CPI-0610 | Multiple myeloma | Phase I |
 TEN-010 | Acute myeloid leukemia | Phase I |
 OTX015 (MK-8628) | Hematologic malignancies | Phase I (completed) |