Table 1.

MDM2/X inhibitor in clinical trails

Inhibitors	Chemical class (first report time)	Chemical structure	Affinity	Population	Identifier /status/phase
RG7112	Imidazoline (2013)		Kd = 2.9 nM	Hematologic neoplasms, advanced solid tumors, PV or ET	NCT00623870 Completed I NCT00559533 Completed I NCT01677780 Completed I NCT01164033 Completed I NCT01605526 Completed I NCT01143740 Completed I NCT01635296 Completed I
RG7388	Imidazoline (2013)		Kd = 0.15 nM	AML, ALL, ET or PV, FL, MM, DLBCL, solid tumors	NCT03287245 Terminated II NCT02545283 Terminated III NCT03362723 Completed I NCT02828930 Completed I NCT02633059 Active, not recruiting I/II NCT03850535 Terminated I/II NCT02407080 Completed I NCT03135262 Terminated I/II NCT02624986 Terminated I/II NCT04029688 Recruiting I/II NCT02670044 Completed I NCT03566485 Terminated I/II NCT04589845 Recruiting II NCT03555149 Active, not recruiting I/II NCT03158389 Recruiting I/II
AMG232	Piperidone (2014)		Kd = 0.045 nM	AML, MM, solid tumors	NCT04640532 Recruiting I/II NCT04835584 Recruiting I/II NCT04502394 Recruiting I/II NCT05027867 Recruiting II NCT04485260 Recruiting I/II NCT03787602 Recruiting I/II NCT04878003 Recruiting II NCT04669067 Recruiting I/II NCT04113616 Recruiting I/II NCT03669965 Active, not recruiting I NCT03217266 Active, not recruiting I NCT03662126 Recruiting II/III NCT04190550 Recruiting I NCT03031730 Recruiting I NCT03107780 Suspended I NCT03041688 Suspended I
SAR405838	Spirooxindole (2014)		Ki = 0.88 nM	Neoplasm malignant	NCT01636479 Completed I NCT01985191 Completed I
NVP-CGM097	Dihydroisoquinoline (2015)		Ki = 1.3 nM	Advanced solid tumors	NCT01760525 Completed I
HDM201	Imidazopyrrolidinone (2016)		In the picomole range	AML, MDS, sarcoma, solid tumors	NCT05180695 Recruiting I/II NCT04496999 Recruiting I NCT03714958 Recruiting I NCT02343172 Completed I NCT02143635 Completed I NCT03940352 Recruiting I NCT03760445 Withdrawn I/II NCT02601378 Terminated I NCT05447663 Not yet recruiting I/II NCT05155709 Recruiting I/II NCT04097821 Suspended I/II NCT04116541 Recruiting I NCT02890069 Completed I
MK-8242	Purine carboxylic acid-derived inhibitor (2016)		IC50 0.07 μM	AML, solid tumors	NCT01451437 Terminated I NCT01463696 Terminated I
DS-3032	Dispiropyrrolidine (2017)		IC50 17.7 ± 5.1 nM	AML, MDS, MM, lymphoma, advanced solid tumor	NCT02579824 Terminated I NCT03634228 Completed I/II NCT03671564 Completed I NCT03552029 Terminated I NCT02319369 Terminated I NCT01877382 Completed I
APG-115	Spirooxindole (2017)		Ki 60 ± 22 nM	AML, CMML, MDS, T-PLL, lymphoma, sarcoma, advanced solid tumor	NCT02935907 Completed I NCT04496349 Recruiting II NCT04785196 Recruiting I/II NCT04358393 Recruiting I/II NCT03611868 Recruiting I/II NCT03781986 Recruiting I/II NCT04275518 Recruiting I
BI-907828	Unknow (2020)	–	IC50 58.52 pM	Liposarcoma, solid tumors	NCT05372367 Recruiting I NCT05376800 Recruiting I NCT05512377 Not yet recruiting II NCT05218499 Recruiting II/III NCT03964233 Recruiting I NCT03449381 Recruiting I
ALRN-6924	Stapled peptide (2018)	–	MDMX Kd 57 nM MDM2 Kd 10.9 nM	AML, MDS, lymphoma, solid tumor	NCT02909972 Completed I NCT03725436 Recruiting I NCT03654716 Recruiting I NCT02264613 Completed I/II NCT04022876 Active, not recruiting I

ALL acute lymphoblastic leukemia, AML acute myeloid leukemia, CMML chronic myelomonocytic leukemia, DLBCL diffuse large B-cell lymphoma, ET essential thrombocythemia, FL follicular lymphoma, MDS myelodysplastic syndrome, MM multiple myeloma, PV polycythemia vera, T-PLL T-prolymphocytic leukemia