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. 2023 Jan 24;16:6. doi: 10.1186/s13045-023-01398-5

Table 2.

Representative small molecules targeting protein degradation under clinical evaluation

Small molecules Target Application Stage of development Refs.
KSQ-4279 USP1 Patients with advanced solid tumors alone or in combination with an oral PARPi Phase I NCT05240898
Perifosine UCHL3 Refractory tumors Phase I or II NCT00873457, NCT01049841, NCT00391560, NCT01097018, NCT00054145
VLX1570 UCHL and USP14 Multiple myeloma Phase II NCT02372240
AMG-232 MDM2 Treating patients with acute myeloid leukemia that has come back (recurrent), does not respond to treatment (refractory), or is newly diagnosed in combination with decitabine Phase I NCT03041688
ALRN-6924 MDM2/MDMX Treatment for resistant (refractory) pediatric cancer Phase I NCT03654716
DS-3032b MDM2 Treatment of relapsed and/or refractory multiple myeloma Phase I NCT02579824
RO6839921 MDM2 Patients with advanced cancers Phase I NCT02098967, NCT01462175
BI 907828 MDM2 Different types of advanced cancer Phase I NCT03449381, NCT05376800, NCT03964233
NX-1607 Cbl-b Advanced malignancies Phase I NCT05107674
KPG-818 CRL4 Hematological malignancies Phase I NCT04283097