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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)