Table 2 Current Pim inhibitors used in vitro, ex vivo, and in current or past clinical trials
From: Targeting Pim kinases in hematological cancers: molecular and clinical review
| Â | Drug Target | Development | Clinical Trials | Treatment Group | Therapy Type |
|---|---|---|---|---|---|
A47 | pan-PIM | Preclinical | – | – | – |
Abemaciclib (Verzenio) | Pim1-CDK4/6 | Phase 1 | NCT03905889: Active (NR) | Metastatic Renal Cell Carcinoma | Dual therapy with Abemaciclib and Sunitinib |
AZD1208 | pan-PIM | Phase 1 Phase 1 | NCT01588548: Completed NCT01489722: Terminated | Adv Solid Tumors/Malignant Lymphoma Relapsed/Refractory AML | Monotherapy Monotherapy |
AZD1897 | pan-PIM | Preclinical | – | – | – |
ETH-155008 | Pim3-CDK4/6 (FLT3) | Phase 1 | NCT04840784: Recruiting | R/R: B-NHL, CLL/SLL and AML | Monotherapy |
ETP-39010 ETP-45299 ETP-47551 | pan-PIM | Preclinical | – | – | – |
INCB053914 (Uzansertib) | pan-PIM | Phase 1 Phase 1/2 Phase 1 | NCT03688152: Completed NCT02587598: Ter/BD NCT04355039: WD/LF | Relapsed/Refractory DLBCL Adv Solid Tumors Relapse/Refractory MM | Dual therapy with INCB050465 Monotherapy and with cytarabine, azacitidine, and ruxolitinib Triple agent therapy with pomalidomide with dexamethasone |
JP11646 | Pim2 | Preclinical | – | – | – |
K00135 | Pim1/Pim2 | Preclinical | – | – | – |
K00486 | Pim1/Pim2 | Preclinical | – | – | – |
LGB321 | pan-PIM | Preclinical | – | – | – |
PIM447 (LGH447) | pan-PIM | Phase 1 Phase 1 Phase 1 Phase 1 Phase 1 | NCT02370706: Completed NCT01456689: Completed NCT02078609: Completed NCT02144038: Completed NCT02160951: Completed | Myelofibrosis Relapsed/Refractory MM AML or High Risk MDS Relapsed/Refractory MM Relapsed/Refractory MM (Japan) | Triple agent therapy with Ruxolitinib and LEE011 Monotherapy Monotherapy or Dual therapy with midostaurin (AML only) Dual agent therapy with BYL719 Monotherapy |
SEL24/MEN1703 (SEL24-B489) | PIM/FLT3 | Phase 1/2 | NCT03008187: Recruiting | AML | Dual Pim/FLT3 therapy |
SGI-1776 | Pim1 | Phase 1 Phase1 | NCT01239108: Withdrawn NCT00848601: Terminated | Relapsed/Refractory Leukemias Refractory Prostate and Refractory NHLs | Monotherapy Monotherapy |
Smi-4a Smi-16a | PIm1 Pim1/Pim2 | Preclinical | – | – | – |
TP-3654 | Pan-PIM | Phase 1/2 | NCT04176198: Recruiting | Intermediate/high-risk primary or secondary MF | Monotherapy |