Table 1 MDM2/X inhibitor in clinical trails
From: Targeting p53 pathways: mechanisms, structures and advances in therapy
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I NCT03714958 Recruiting I NCT02343172 Completed I NCT02143635 Completed I NCT03940352 Recruiting I NCT03760445 Withdrawn I/II NCT02601378 Terminated I NCT05447663 Not yet recruiting I/II NCT05155709 Recruiting I/II NCT04097821 Suspended I/II NCT04116541 Recruiting I NCT02890069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 |
