Table 2 Examples of small-molecule development candidates identified against PPIs in cancer treatment
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) | Extensive-stage small cell lung cancer | 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) |