Idasanutlin
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Also known as IdasanutlinaIdasanutlineRG-7388RG7388RO-5503781RO5503781UNII-QSQ883V35UIDASANUTLIN (RG-7388)
Summary
Idasanutlin (CHEMBL2402737) is a phase-3 clinical-stage small molecule; indicated across 11 conditions including acute myeloid leukemia and neoplasm.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Indications: 11 conditions
- Clinical trials: 17
- Chemistry: 616.5 Da · C31H29Cl2F2N3O4
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL2402737 |
| Name | Idasanutlin |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 53358942 |
| Molecular formula | C31H29Cl2F2N3O4 |
| Molecular weight | 616.5 |
| InChIKey | TVTXCJFHQKSQQM-LJQIRTBHSA-N |
SMILES: CC(C)(C)C[C@H]1[C@]([C@H]([C@@H](N1)C(=O)NC2=C(C=C(C=C2)C(=O)O)OC)C3=C(C(=CC=C3)Cl)F)(C#N)C4=C(C=C(C=C4)Cl)F
IUPAC name: 4-[[(2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)pyrrolidine-2-carbonyl]amino]-3-methoxybenzoic acid
Also known as: Idasanutlin, Idasanutlina, Idasanutline, RG-7388, RG7388, RO-5503781, RO5503781, IDASANUTLIN, UNII-QSQ883V35U, IDASANUTLINE, IDASANUTLINA, IDASANUTLIN (RG-7388)
Patent coverage: 585 distinct patent families (1,511 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 1,084 (72%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Tumour suppressor p53/oncoprotein Mdm2, E3 ubiquitin-protein ligase Mdm2.
Bioactivity
ChEMBL activities: 7 potent at pChembl ≥ 5 of 7 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| MDM2 | 9.82 | Kd | 0.15 | nM | CHEMBL_ACT_13953120 |
| MDM2 | 8.22 | IC50 | 6 | nM | CHEMBL_ACT_13368065 |
| MDM2 | 8.22 | IC50 | 6 | nM | CHEMBL_ACT_19044305 |
| TP53 | 8.22 | IC50 | 6 | nM | CHEMBL_ACT_25030019 |
| TP53 | 8.05 | IC50 | 9 | nM | CHEMBL_ACT_14998193 |
| MDM2 | 8.01 | Kd | 9.8 | nM | CHEMBL_ACT_24343804 |
| TP53 | 8 | IC50 | 10 | nM | CHEMBL_ACT_14998218 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
11 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| acute myeloid leukemia | 3 | MONDO:0018874 | EFO:0000222 |
| neoplasm | 2 | MONDO:0005070 | EFO:0000616 |
| acquired polycythemia vera | 2 | MONDO:0009891 | EFO:0002429 |
| diffuse large B-cell lymphoma | 1 | MONDO:0018905 | EFO:0000403 |
| glioblastoma | 1 | MONDO:0018177 | EFO:0000519 |
| plasma cell myeloma | 1 | MONDO:0009693 | EFO:0001378 |
| non-Hodgkin lymphoma | 1 | MONDO:0018908 | EFO:0005952 |
| essential thrombocythemia | 1 | MONDO:0005029 | EFO:0000479 |
| breast neoplasm | 1 | MONDO:0021100 | MONDO:0007254 |
| follicular lymphoma | 1 | MONDO:0018906 | MONDO:0018906 |
| colorectal neoplasm | 1 | MONDO:0005335 | MONDO:0005575 |
Clinical trials
Total trials: 17.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE1/PHASE2 | 8 |
| PHASE1 | 7 |
| PHASE3 | 1 |
| PHASE2 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT02545283 | PHASE3 | TERMINATED | A Study of Idasanutlin With Cytarabine Versus Cytarabine Plus Placebo in Participants With Relapsed or Refractory Acute Myeloid Leukemia (AML) |
| NCT02624986 | PHASE1/PHASE2 | TERMINATED | A Study of Idasanutlin in Combination With Obinutuzumab in Relapsed/Refractory (R/R) Follicular Lymphoma (FL) and in Combination With Rituximab in R/R Diffuse Large B-Cell Lymphoma (DLBCL) Participants |
| NCT02633059 | PHASE1/PHASE2 | COMPLETED | Idasanutlin, Ixazomib Citrate, and Dexamethasone in Treating Patients With Relapsed Multiple Myeloma |
| NCT03135262 | PHASE1/PHASE2 | TERMINATED | A Study of Obinutuzumab in Combination With Idasanutlin and Venetoclax in Participants With Relapsed or Refractory (R/R) Follicular Lymphoma (FL) or Rituximab in Combination With Idasanutlin and Venetoclax in Participants With R/R Diffuse Large B-Cell Lymphoma (DLBCL) |
| NCT03158389 | PHASE1/PHASE2 | COMPLETED | NCT Neuro Master Match - N²M² (NOA-20) |
| NCT03287245 | PHASE2 | TERMINATED | A Study to Evaluate the Efficacy, Safety, Pharmacokinetics and Pharmacodynamics of Idasanutlin Monotherapy in Participants With Hydroxyurea-Resistant/Intolerant Polycythemia Vera |
| NCT03555149 | PHASE1/PHASE2 | TERMINATED | A Study Evaluating the Efficacy and Safety of Multiple Immunotherapy-Based Treatment Combinations in Patients With Metastatic Colorectal Cancer (Morpheus-CRC) |
| NCT03566485 | PHASE1/PHASE2 | TERMINATED | Atezolizumab and Cobimetinib or Idasanutlin in Participants With Stage IV or Unresectable Recurrent Estrogen Receptor Positive Breast Cancer |
| NCT03850535 | PHASE1/PHASE2 | TERMINATED | A Study Evaluating the Safety and Efficacy of Idasanutlin in Combination With Cytarabine and Daunorubicin in Patients Newly Diagnosed With Acute Myeloid Leukemia (AML) and the Safety and Efficacy of Idasanutlin in the Maintenance of First AML Complete Remission |
| NCT04029688 | PHASE1/PHASE2 | TERMINATED | A Study Evaluating the Safety, Tolerability, Pharmacokinetics and Preliminary Activity of Idasanutlin in Combination With Either Chemotherapy or Venetoclax in Treatment of Pediatric and Young Adult Participants With Relapsed/Refractory Acute Leukemias or Solid Tumors |
| NCT01462175 | PHASE1 | COMPLETED | A First-In-Human Study of RO5503781 in Participants With Advanced Malignancies Except Leukemia |
| NCT01901172 | PHASE1 | COMPLETED | A Study of the Drug-Drug Interaction of RO5503781 and Posaconazole, the Relative Bioavailability of New Formulations of RO5503781 and the Food-Effect on the Pharmacokinetics of RO5503781 in Patients With Solid Tumors |
| NCT02407080 | PHASE1 | COMPLETED | Open Label Study of Single Agent Oral RG7388 in Patients With Polycythemia Vera and Essential Thrombocythemia |
| NCT02670044 | PHASE1 | COMPLETED | A Study of Venetoclax in Combination With Cobimetinib and Venetoclax in Combination With Idasanutlin in Patients With Relapsed or Refractory Acute Myeloid Leukemia Who Are Not Eligible for Cytotoxic Therapy |
| NCT02828930 | PHASE1 | COMPLETED | A Study to Determine the Excretion Balance, Pharmacokinetics, Metabolism and Absolute Oral Bioavailability of a Single Oral Dose of [14C]-Labeled Idasanutlin and an Intravenous Tracer Dose of [13C]-Labeled Idasanutlin in a Single Cohort of Participants With Solid Tumors (Malignancies) |
| NCT03362723 | PHASE1 | COMPLETED | A Study to Investigate the Bioequivalence or Relative Bioavailability of Three New Idasanutlin Tablet Variants Following Oral Administration in Participants With Solid Tumors |
| NCT05952687 | PHASE1 | WITHDRAWN | Trial of Idasanutlin and Selinexor Therapy for Children With Progressive/Relapsed AT/RT or Extra-CNS Malignant Rhabdoid Tumors |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).
Related Atlas pages
- Diseases: acute myeloid leukemia