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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)