Alvocidib
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Also known as Alvocidib freebaseFlavopiridolHL 275HL-275HMR 1275HMR-1275L 86 8275L-868275MDL 107,826AMDL-107826ANSC-649890AlvocidibFLAVOPIRIDOL_ALVOCIDIB
Summary
Alvocidib (CHEMBL428690) is a phase-3 clinical-stage small-molecule antineoplastic agent targeting CDK2 and CDK4; indicated across 19 conditions including lymphoma and plasma cell myeloma.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Targets: 2 (CDK2, CDK4)
- Indications: 19 conditions
- Clinical trials: 58
- Chemistry: 401.8 Da · C21H20ClNO5
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL428690 |
| Name | Alvocidib |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 5287969 |
| ChEBI | CHEBI:47344 |
| Molecular formula | C21H20ClNO5 |
| Molecular weight | 401.8 |
| InChIKey | BIIVYFLTOXDAOV-YVEFUNNKSA-N |
SMILES: CN1CC[C@@H]([C@@H](C1)O)C2=C(C=C(C3=C2OC(=CC3=O)C4=CC=CC=C4Cl)O)O
IUPAC name: 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]chromen-4-one
ChEBI definition: A synthetic dihydroxyflavone that is 5,7-dihydroxyflavone which is substituted by a 3-hydroxy-1-methylpiperidin-4-yl group at position 8 and by a chlorine at the 2’ position (the (−)-3S,4R stereoisomer). A cyclin-dependent kinase 9 (CDK9) inhibitor, it has been studied for the treatment of acute myeloid leukaemia, arthritis and atherosclerotic plaque formation.
Pharmacological roles (ChEBI): antineoplastic agent, EC 2.7.11.22 (cyclin-dependent kinase) inhibitor, antirheumatic drug, apoptosis inducer.
Also known as: Alvocidib, Alvocidib freebase, Flavopiridol, HL 275, HL-275, HMR 1275, HMR-1275, L 86 8275, L-868275, MDL 107,826A, MDL-107826A, NSC-649890
Parent form; salt/anhydrous children: CHEMBL2105698
Patent coverage: 7,239 distinct patent families (27,781 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 24,608 (89%) 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
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| CDK2 | cyclin dependent kinase 2 | Inhibition | 7 | 71.1% | P24941 |
| CDK4 | cyclin dependent kinase 4 | Inhibition | 7.19 | 58% | P11802 |
Broader ChEMBL bioactivity targets: 179 (assay-derived). Sample: Leucine-rich repeat serine/threonine-protein kinase 2, Rhodopsin kinase GRK7, Homeodomain-interacting protein kinase 4, Serine/threonine-protein kinase TAO2, Dual specificity protein kinase CLK1, Serine/threonine-protein kinase MAK, Cyclin-dependent kinase-like 5, Serine/threonine-protein kinase ICK, Serine/threonine-protein kinase VRK2, Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma, Bromodomain testis-specific protein, Cyclin-dependent kinase 13, Receptor tyrosine-protein kinase erbB-2, Macrophage colony-stimulating factor 1 receptor, Tyrosine-protein kinase ABL1, Cyclin-dependent kinase 5/CDK5 activator 1, Cyclin-dependent kinase 4/cyclin D1, Cyclin-dependent kinase 1/cyclin B1, Cyclin-dependent kinase 2/cyclin E1, Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma.
Bioactivity
ChEMBL activities: 511 potent at pChembl ≥ 5 of 521 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| CILK1 | 9.16 | Kd | 0.69 | nM | CHEMBL_ACT_7579762 |
| CCNT1 | 9.15 | Ki | 0.7 | nM | CHEMBL_ACT_29064286 |
| CCNT1 | 8.85 | IC50 | 1.4 | nM | CHEMBL_ACT_29064281 |
| CCNT1 | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_16737181 |
| CDK9 | 8.52 | Ki | 3 | nM | CHEMBL_ACT_12622859 |
| CCNT1 | 8.52 | Ki | 3 | nM | CHEMBL_ACT_12622894 |
| LARP7 | 8.52 | Ki | 3 | nM | CHEMBL_ACT_19112063 |
| CDK9 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_22758226 |
| CDK9 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_24975154 |
| CDK9 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_25539593 |
| CDK4 | 8.48 | Kd | 3.3 | nM | CHEMBL_ACT_7579447 |
| CCNT1 | 8.43 | IC50 | 3.7 | nM | CHEMBL_ACT_18146977 |
| CDK9 | 8.35 | IC50 | 4.5 | nM | CHEMBL_ACT_25611224 |
| CCNT1 | 8.34 | IC50 | 4.59 | nM | CHEMBL_ACT_16385312 |
| CCNT1 | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_26327842 |
| CCNT1 | 8.22 | IC50 | 6 | nM | CHEMBL_ACT_14659236 |
| CDK17 | 8.22 | Kd | 6 | nM | CHEMBL_ACT_17889582 |
| CCNT1 | 8.22 | IC50 | 6 | nM | CHEMBL_ACT_26224807 |
| CDK9 | 8.21 | IC50 | 6.1 | nM | CHEMBL_ACT_26163137 |
| CDK9 | 8.19 | Kd | 6.4 | nM | CHEMBL_ACT_2903861 |
| CCNT1 | 8.19 | Kd | 6.4 | nM | CHEMBL_ACT_29064328 |
| CDK9 | 8.19 | Kd | 6.4 | nM | CHEMBL_ACT_7579497 |
| CDK9 | 8.15 | Kd | 7 | nM | CHEMBL_ACT_17891286 |
| CDKL5 | 8.15 | Kd | 7.1 | nM | CHEMBL_ACT_7579572 |
| CDK4 | 8.05 | Kd | 9 | nM | CHEMBL_ACT_7579446 |
| CDK7 | 8 | IC50 | 10 | nM | CHEMBL_ACT_22758219 |
| CDK4 | 8 | IC50 | 10 | nM | CHEMBL_ACT_24788462 |
| CDK1 | 8 | IC50 | 10 | nM | CHEMBL_ACT_24788532 |
| CDK2 | 8 | IC50 | 10 | nM | CHEMBL_ACT_24788536 |
| CDK9 | 8 | IC50 | 10 | nM | CHEMBL_ACT_24788541 |
| CDK7 | 8 | IC50 | 10 | nM | CHEMBL_ACT_24975193 |
| CDK7 | 8 | IC50 | 10 | nM | CHEMBL_ACT_25539597 |
| CDK9 | 8 | IC50 | 10 | nM | CHEMBL_ACT_25980885 |
| CCNT1 | 7.96 | IC50 | 11 | nM | CHEMBL_ACT_16737224 |
| CCNT1 | 7.96 | IC50 | 11 | nM | CHEMBL_ACT_22967903 |
| CCNT1 | 7.96 | IC50 | 11 | nM | CHEMBL_ACT_26281857 |
| CAMKK1 | 7.72 | Kd | 19 | nM | CHEMBL_ACT_1650008 |
| CCNT1 | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_18224282 |
| CDK9 | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_18784877 |
| CDK9 | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_19027223 |
| CDK4 | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_19112058 |
| CCNT1 | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_19112061 |
| CDK9 | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_19258241 |
| CDK9 | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_22967931 |
| CDK4 | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_24759546 |
| CCNT1 | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_24759587 |
| CDK1 | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_24993209 |
| CDK2 | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_24993215 |
| CDK4 | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_24993230 |
| CDK6 | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_24993236 |
| CDK9 | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_24993240 |
| CDK9 | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_25062192 |
| CDK9 | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_3420190 |
| CDK7 | 7.64 | Kd | 23 | nM | CHEMBL_ACT_2903823 |
| CDK7 | 7.64 | Kd | 23 | nM | CHEMBL_ACT_7579512 |
| CDK1 | 7.57 | IC50 | 27 | nM | CHEMBL_ACT_16737218 |
| MAK | 7.55 | Kd | 28 | nM | CHEMBL_ACT_7579695 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_13914204 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_16610777 |
| CCNB2 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_182052 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_18784880 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_19027200 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_19112054 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_19258236 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_224601 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_22758192 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_22930617 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_24708390 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_24789101 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_24975167 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_24984402 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_25062180 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_25073415 |
| CCNB2 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_253440 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_25539583 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_25980855 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_29252794 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_3420187 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_3438052 |
| CDK1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_3446977 |
| CCNB2 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_522220 |
| TYK2 | 7.46 | Kd | 35 | nM | CHEMBL_ACT_7579580 |
| CDK4 | 7.42 | IC50 | 38 | nM | CHEMBL_ACT_26327830 |
| CDK2 | 7.4 | Ki | 40 | nM | CHEMBL_ACT_19112048 |
| CDK1 | 7.4 | Ki | 40 | nM | CHEMBL_ACT_19112064 |
| CDK4 | 7.4 | Ki | 40 | nM | CHEMBL_ACT_19112065 |
| CDK4 | 7.4 | IC50 | 40 | nM | CHEMBL_ACT_26281851 |
| CDK2 | 7.4 | IC50 | 40 | nM | CHEMBL_ACT_3420188 |
| CDK1 | 7.39 | Ki | 41 | nM | CHEMBL_ACT_26224832 |
| CDK5 | 7.37 | Kd | 43 | nM | CHEMBL_ACT_1650017 |
| CDK4 | 7.26 | EC50 | 55 | nM | CHEMBL_ACT_26281885 |
| TNNI3K | 7.26 | Kd | 55 | nM | CHEMBL_ACT_2896731 |
| TNNI3K | 7.26 | Kd | 55 | nM | CHEMBL_ACT_7581691 |
| EIF2AK1 | 7.24 | Kd | 58 | nM | CHEMBL_ACT_17898665 |
| CDK19 | 7.24 | Kd | 57 | nM | CHEMBL_ACT_2901375 |
| CDK19 | 7.24 | Kd | 57 | nM | CHEMBL_ACT_7581688 |
| CDK5 | 7.22 | IC50 | 60 | nM | CHEMBL_ACT_10882649 |
| CDK6 | 7.22 | IC50 | 60 | nM | CHEMBL_ACT_22758217 |
| CDK6 | 7.22 | IC50 | 60 | nM | CHEMBL_ACT_24789028 |
| CDK6 | 7.22 | IC50 | 60 | nM | CHEMBL_ACT_24975150 |
Target pathways
Aggregated over 2 target gene(s): CDK2, CDK4.
Top Reactome pathways
94 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Developmental Biology | 2 | CDK2, CDK4 |
| Reproduction | 2 | CDK2, CDK4 |
| Meiosis | 2 | CDK2, CDK4 |
| Signal Transduction | 2 | CDK2, CDK4 |
| Cell Cycle | 2 | CDK2, CDK4 |
| Disease | 2 | CDK2, CDK4 |
| SCF(Skp2)-mediated degradation of p27/p21 | 2 | CDK2, CDK4 |
| Generic Transcription Pathway | 2 | CDK2, CDK4 |
| Cellular responses to stress | 2 | CDK2, CDK4 |
| Senescence-Associated Secretory Phenotype (SASP) | 2 | CDK2, CDK4 |
| Cellular Senescence | 2 | CDK2, CDK4 |
| Mitotic G1 phase and G1/S transition | 2 | CDK2, CDK4 |
| Cyclin E associated events during G1/S transition | 2 | CDK2, CDK4 |
| G1/S Transition | 2 | CDK2, CDK4 |
| Cyclin D associated events in G1 | 2 | CDK2, CDK4 |
| G1 Phase | 2 | CDK2, CDK4 |
| S Phase | 2 | CDK2, CDK4 |
| Cell Cycle, Mitotic | 2 | CDK2, CDK4 |
| Cyclin A:Cdk2-associated events at S phase entry | 2 | CDK2, CDK4 |
| RNA Polymerase II Transcription | 2 | CDK2, CDK4 |
| Gene expression (Transcription) | 2 | CDK2, CDK4 |
| Signaling by PTK6 | 2 | CDK2, CDK4 |
| PTK6 Regulates Cell Cycle | 2 | CDK2, CDK4 |
| Cellular responses to stimuli | 2 | CDK2, CDK4 |
| Signaling by Non-Receptor Tyrosine Kinases | 2 | CDK2, CDK4 |
| Meiotic recombination | 2 | CDK2, CDK4 |
| Transcriptional regulation of granulopoiesis | 2 | CDK2, CDK4 |
| Aberrant regulation of mitotic G1/S transition in cancer due to RB1 defects | 2 | CDK2, CDK4 |
| Defective binding of RB1 mutants to E2F1,(E2F2, E2F3) | 2 | CDK2, CDK4 |
| Diseases of mitotic cell cycle | 2 | CDK2, CDK4 |
| Aberrant regulation of mitotic cell cycle due to RB1 defects | 2 | CDK2, CDK4 |
| Hemostasis | 1 | CDK2 |
| G0 and Early G1 | 1 | CDK2 |
| Telomere Maintenance | 1 | CDK2 |
| Telomere Extension By Telomerase | 1 | CDK2 |
| APC/C-mediated degradation of cell cycle proteins | 1 | CDK2 |
| Activation of ATR in response to replication stress | 1 | CDK2 |
| Regulation of APC/C activators between G1/S and early anaphase | 1 | CDK2 |
| Extension of Telomeres | 1 | CDK2 |
| Oxidative Stress Induced Senescence | 1 | CDK4 |
| Oncogene Induced Senescence | 1 | CDK4 |
| DNA Damage/Telomere Stress Induced Senescence | 1 | CDK2 |
| RMTs methylate histone arginines | 1 | CDK4 |
| Chromatin modifying enzymes | 1 | CDK4 |
| Transcriptional Regulation by TP53 | 1 | CDK2 |
| Transcriptional regulation of white adipocyte differentiation | 1 | CDK4 |
| Mitotic G2-G2/M phases | 1 | CDK2 |
| Regulation of mitotic cell cycle | 1 | CDK2 |
| Chromatin organization | 1 | CDK4 |
| Regulation of TP53 Activity | 1 | CDK2 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| G1/S transition of mitotic cell cycle | 2 |
| protein phosphorylation | 2 |
| signal transduction | 2 |
| positive regulation of cell population proliferation | 2 |
| regulation of G2/M transition of mitotic cell cycle | 2 |
| regulation of gene expression | 2 |
| cell division | 2 |
| G2/M transition of mitotic cell cycle | 1 |
| negative regulation of transcription by RNA polymerase II | 1 |
| DNA replication | 1 |
| DNA repair | 1 |
| chromatin remodeling | 1 |
| DNA-templated transcription | 1 |
| potassium ion transport | 1 |
| centriole replication | 1 |
Indications & clinical
Indications
16 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.
| Disease (in trials) | Phase | MONDO | EFO |
|---|---|---|---|
| lymphoma | 2 | MONDO:0005062 | EFO:0000574 |
| plasma cell myeloma | 2 | MONDO:0009693 | EFO:0001378 |
| B-cell chronic lymphocytic leukemia | 2 | MONDO:0004948 | EFO:0000095 |
| acute myeloid leukemia | 2 | MONDO:0018874 | EFO:0000222 |
| cutaneous melanoma | 2 | MONDO:0005012 | EFO:0000389 |
| sarcoma | 2 | MONDO:0005089 | EFO:0000691 |
| prolymphocytic leukemia | 2 | MONDO:0001023 | MONDO:0001023 |
| kidney cancer | 2 | MONDO:0002367 | MONDO:0002367 |
| endometrium neoplasm | 2 | MONDO:0021251 | MONDO:0011962 |
| exocrine pancreatic carcinoma | 2 | MONDO:0005192 | EFO:0002618 |
| neoplasm | 1 | MONDO:0005070 | EFO:0000616 |
| lymphoid neoplasm | 1 | MONDO:0005157 | EFO:0001642 |
| leukemia | 1 | MONDO:0005059 | EFO:0000565 |
| male breast carcinoma | 1 | MONDO:0005628 | EFO:0006861 |
| breast neoplasm | 1 | MONDO:0021100 | MONDO:0007254 |
| lymphoid leukemia | 1 | MONDO:0005402 | EFO:0004289 |
3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 58.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE1 | 30 |
| PHASE2 | 23 |
| PHASE1/PHASE2 | 5 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00003039 | PHASE2 | COMPLETED | Flavopiridol in Treating Patients With Recurrent Intermediate-Grade or High-Grade Non-Hodgkin’s Lymphoma or Mantle Cell Lymphoma |
| NCT00003256 | PHASE2 | COMPLETED | Flavopiridol in Treating Patients With Recurrent Prostate Cancer |
| NCT00003620 | PHASE2 | COMPLETED | Flavopiridol in Treating Patients With Chronic Lymphocytic Leukemia |
| NCT00005074 | PHASE2 | COMPLETED | Flavopiridol in Treating Patients With Previously Untreated or Relapsed Mantle Cell Lymphoma |
| NCT00005971 | PHASE2 | COMPLETED | Flavopiridol in Treating Patients With Metastatic Malignant Melanoma |
| NCT00005974 | PHASE2 | COMPLETED | Flavopiridol in Treating Patients With Recurrent, Locally Advanced, or Metastatic Soft Tissue Sarcoma |
| NCT00006245 | PHASE2 | COMPLETED | Flavopiridol and Paclitaxel in Treating Patients With Locally Advanced or Metastatic Esophageal Cancer That Has Not Responded to Previous Paclitaxel |
| NCT00016016 | PHASE1/PHASE2 | COMPLETED | Flavopiridol, Cytarabine, and Mitoxantrone in Treating Patients With Acute Leukemia |
| NCT00016939 | PHASE2 | COMPLETED | Flavopiridol in Treating Patients With Unresectable or Metastatic Kidney Cancer |
| NCT00020189 | PHASE2 | COMPLETED | Flavopiridol in Treating Patients With Recurrent or Metastatic Head and Neck Cancer |
| NCT00020332 | PHASE1/PHASE2 | COMPLETED | Docetaxel and Flavopiridol in Treating Patients With Locally Advanced or Metastatic Breast Cancer |
| NCT00023894 | PHASE2 | COMPLETED | Flavopiridol in Treating Patients With Recurrent or Persistent Endometrial Cancer |
| NCT00047203 | PHASE2 | COMPLETED | Flavopiridol in Treating Patients With Relapsed or Refractory Multiple Myeloma |
| NCT00058240 | PHASE1/PHASE2 | COMPLETED | Flavopiridol in Treating Patients With Previously Treated Chronic Lymphocytic Leukemia or Lymphocytic Lymphoma |
| NCT00083122 | PHASE2 | COMPLETED | Cisplatin and Flavopiridol in Treating Patients With Advanced Ovarian Epithelial Cancer or Primary Peritoneal Cancer |
| NCT00087282 | PHASE2 | COMPLETED | Irinotecan and Flavopiridol in Treating Patients With Advanced Liver Cancer |
| NCT00098371 | PHASE2 | TERMINATED | Flavopiridol in Treating Patients With Chronic Lymphocytic Leukemia or Prolymphocytic Leukemia |
| NCT00112723 | PHASE1/PHASE2 | TERMINATED | Flavopiridol in Treating Patients With Relapsed or Refractory Lymphoma or Multiple Myeloma |
| NCT00331682 | PHASE2 | COMPLETED | Docetaxel and Flavopiridol in Treating Patients With Refractory Metastatic Pancreatic Cancer |
| NCT00407966 | PHASE2 | COMPLETED | Alvocidib, Cytarabine, and Mitoxantrone in Treating Patients With Newly Diagnosed Acute Myeloid Leukemia |
| NCT00445341 | PHASE1/PHASE2 | COMPLETED | Flavopiridol to Treat Relapsed Mantle Cell Lymphoma or Diffuse Large B-Cell Lymphoma |
| NCT00464633 | PHASE2 | COMPLETED | Alvocidib in Patients With Previously Treated Chronic Lymphocytic Leukemia or Prolymphocytic Leukemia Arising From Chronic Lymphocytic Leukemia (CLL) |
| NCT00634244 | PHASE2 | COMPLETED | Comparing Three Different Combination Chemotherapy Regimens in Treating Patients With Relapsed or Refractory Acute Myeloid Leukemia |
| NCT00795002 | PHASE2 | COMPLETED | Alvocidib, Cytarabine, and Mitoxantrone in Treating Patients With Newly Diagnosed Acute Myeloid Leukemia |
| NCT00991952 | PHASE2 | COMPLETED | Irinotecan Hydrochloride With or Without Alvocidib in Treating Patients With Advanced Stomach or Gastroesophageal Junction Cancer That Cannot Be Removed By Surgery |
| NCT01349972 | PHASE2 | COMPLETED | Alvocidib, Cytarabine, and Mitoxantrone Hydrochloride or Cytarabine and Daunorubicin Hydrochloride in Treating Patients With Newly Diagnosed Acute Myeloid Leukemia |
| NCT02520011 | PHASE2 | TERMINATED | Alvocidib Biomarker-driven Phase 2 AML Study |
| NCT03969420 | PHASE2 | TERMINATED | Study of Alvocidib in Patients With Relapsed/Refractory AML Following Treatment With Venetoclax Combination Therapy |
| NCT00003004 | PHASE1 | COMPLETED | Combination Chemotherapy in Treating Patients With Refractory or Recurrent Solid Tumors |
| NCT00003690 | PHASE1 | COMPLETED | Flavopiridol Plus Cisplatin or Carboplatin in Treating Patients With Advanced Solid Tumors |
| NCT00006485 | PHASE1 | COMPLETED | Flavopiridol and Irinotecan in Treating Patients With Advanced Solid Tumors |
| NCT00007917 | PHASE1 | COMPLETED | Gemcitabine Plus Flavopiridol in Treating Patients With Advanced Solid Tumors |
| NCT00012181 | PHASE1 | COMPLETED | Flavopiridol in Treating Children With Relapsed or Refractory Solid Tumors or Lymphomas |
| NCT00016185 | PHASE1 | COMPLETED | Flavopiridol and Docetaxel in Treating Patients With Advanced Solid Tumors |
| NCT00019344 | PHASE1 | COMPLETED | Flavopiridol in Treating Patients With Refractory Cancer |
| NCT00021073 | PHASE1 | COMPLETED | Combination Chemotherapy in Treating Patients With Advanced Cancer |
| NCT00039455 | PHASE1 | TERMINATED | Trastuzumab and Flavopiridol in Treating Patients With Metastatic Breast Cancer |
| NCT00042874 | PHASE1 | COMPLETED | Combination Chemotherapy in Treating Patients With Locally Advanced or Metastatic Solid Tumors |
| NCT00045448 | PHASE1 | COMPLETED | Combination Chemotherapy in Treating Patients With Advanced Solid Tumors |
| NCT00046917 | PHASE1 | COMPLETED | Combination Chemotherapy in Treating Patients With Advanced Solid Tumors |
| NCT00047307 | PHASE1 | COMPLETED | Flavopiridol Plus Radiation Therapy Followed By Gemcitabine Hydrochloride in Treating Patients With Locally Advanced, Unresectable Pancreatic Cancer |
| NCT00058227 | PHASE1 | COMPLETED | Alvocidib, Fludarabine Phosphate, and Rituximab in Treating Patients With Lymphoproliferative Disorders or Mantle Cell Lymphoma |
| NCT00064285 | PHASE1 | COMPLETED | Flavopiridol and Imatinib Mesylate in Treating Patients With Hematologic Cancer |
| NCT00070239 | PHASE1 | TERMINATED | Alvocidib in Treating Patients With Metastatic or Unresectable Refractory Solid Tumors or Hematologic Malignancies |
| NCT00072436 | PHASE1 | COMPLETED | Gemcitabine Hydrochloride and Alvocidib in Treating Patients With Solid Tumors |
| NCT00079352 | PHASE1 | COMPLETED | Flavopiridol, Gemcitabine, and Irinotecan in Treating Patients With Unresectable or Metastatic Solid Tumors |
| NCT00080990 | PHASE1 | COMPLETED | Alvocidib, Oxaliplatin, Fluorouracil, and Leucovorin Calcium in Treating Patients With Advanced Solid Tumors |
| NCT00094978 | PHASE1 | TERMINATED | Depsipeptide/Flavopiridol Infusion for Cancers of the Lungs, Esophagus, Pleura, Thymus or Mediastinum |
| NCT00098579 | PHASE1 | COMPLETED | Doxorubicin Hydrochloride and Alvocidib in Treating Patients With Metastatic or Recurrent Sarcoma That Cannot Be Removed By Surgery |
| NCT00101231 | PHASE1 | TERMINATED | Flavopiridol in Treating Patients With Relapsed or Refractory Acute Myeloid Leukemia, Acute Lymphoblastic Leukemia, or Chronic Myelogenous Leukemia |
| NCT00112684 | PHASE1 | TERMINATED | Alvocidib in Treating Patients With Locally Advanced or Metastatic Solid Tumors |
| NCT00278330 | PHASE1 | COMPLETED | Flavopiridol and Vorinostat in Treating Patients With Relapsed or Refractory Acute Leukemia or Chronic Myelogenous Leukemia or Refractory Anemia |
| NCT00324480 | PHASE1 | COMPLETED | Vorinostat and Alvocidib in Treating Patients With Advanced Solid Tumors |
| NCT00377104 | PHASE1 | TERMINATED | Alvocidib in Treating Patients With B-Cell Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma |
| NCT00470197 | PHASE1 | COMPLETED | Flavopiridol, Cytarabine, and Mitoxantrone in Treating Patients With Relapsed or Refractory Acute Leukemia |
| NCT03298984 | PHASE1 | COMPLETED | Ph I Study of Alvocidib and Cytarabine/Daunorubicin (7+3) in Patients With Newly Diagnosed Acute Myeloid Leukemia (AML). |
| NCT03441555 | PHASE1 | COMPLETED | A Study of Venetoclax and Alvocidib in Patients With Relapsed/Refractory Acute Myeloid Leukemia |
| NCT03563560 | PHASE1 | COMPLETED | A Study of DSP-2033 (Alvocidib) in Patients With Acute Myeloid Leukemia |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
86 molecules share ≥1 primary target. Top 86 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| ABEMACICLIB | ChEMBL | Phase 4 (approved) | CDK2, CDK4 |
| CERITINIB | ChEMBL | Phase 4 (approved) | CDK2, CDK4 |
| DABRAFENIB | ChEMBL | Phase 4 (approved) | CDK2, CDK4 |
| GILTERITINIB | ChEMBL | Phase 4 (approved) | CDK2, CDK4 |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | CDK2, CDK4 |
| PALBOCICLIB | ChEMBL | Phase 4 (approved) | CDK2, CDK4 |
| RIBOCICLIB | ChEMBL | Phase 4 (approved) | CDK2, CDK4 |
| TRILACICLIB | ChEMBL | Phase 4 (approved) | CDK2, CDK4 |
| DINACICLIB | ChEMBL | Phase 3 | CDK2, CDK4 |
| LEROCICLIB | ChEMBL | Phase 3 | CDK2, CDK4 |
| LESTAURTINIB | ChEMBL | Phase 3 | CDK2, CDK4 |
| QUERCETIN | ChEMBL | Phase 3 | CDK2, CDK4 |
| AT-7519 | ChEMBL | Phase 2 | CDK2, CDK4 |
| CROZBACICLIB | ChEMBL | Phase 2 | CDK2, CDK4 |
| CT-7001 | ChEMBL | Phase 2 | CDK2, CDK4 |
| CULMERCICLIB | ChEMBL | Phase 2 | CDK2, CDK4 |
| CYC-065 | ChEMBL | Phase 2 | CDK2, CDK4 |
| EBVACICLIB | ChEMBL | Phase 2 | CDK2, CDK4 |
| ELLAGIC ACID | ChEMBL | Phase 2 | CDK2, CDK4 |
| INDIRUBIN | ChEMBL | Phase 2 | CDK2, CDK4 |
| INIXACICLIB | ChEMBL | Phase 2 | CDK2, CDK4 |
| ISTISOCICLIB | ChEMBL | Phase 2 | CDK2, CDK4 |
| LY-2090314 | ChEMBL | Phase 2 | CDK2, CDK4 |
| MILCICLIB | ChEMBL | Phase 2 | CDK2, CDK4 |
| NARAZACICLIB | ChEMBL | Phase 2 | CDK2, CDK4 |
| REBASTINIB | ChEMBL | Phase 2 | CDK2, CDK4 |
| RG-547 | ChEMBL | Phase 2 | CDK2, CDK4 |
| RIVICICLIB | ChEMBL | Phase 2 | CDK2, CDK4 |
| RONICICLIB | ChEMBL | Phase 2 | CDK2, CDK4 |
| SELICICLIB | ChEMBL | Phase 2 | CDK2, CDK4 |
| TEGTOCICLIB | ChEMBL | Phase 2 | CDK2, CDK4 |
| ULECACICLIB | ChEMBL | Phase 2 | CDK2, CDK4 |
| VORUCICLIB | ChEMBL | Phase 2 | CDK2, CDK4 |
| ZEMIRCICLIB | ChEMBL | Phase 2 | CDK2, CDK4 |
| Afatinib | PubChem | Approved | CDK2, CDK4 |
| Binimetinib | PubChem | Approved | CDK2, CDK4 |
| Crizotinib | PubChem | Approved | CDK2, CDK4 |
| dacomitinib | PubChem | Approved | CDK2, CDK4 |
| Fostamatinib | PubChem | Approved | CDK2, CDK4 |
| Idelalisib | PubChem | Approved | CDK2, CDK4 |
| Pazopanib | PubChem | Approved | CDK2, CDK4 |
| regorafenib | PubChem | Approved | CDK2, CDK4 |
| Selumetinib | PubChem | Approved | CDK2, CDK4 |
| Trametinib | PubChem | Approved | CDK2, CDK4 |
| ENCORAFENIB | ChEMBL | Phase 4 (approved) | CDK4 |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | CDK2 |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | CDK4 |
| LAPATINIB | ChEMBL | Phase 4 (approved) | CDK2 |
| MOMELOTINIB | ChEMBL | Phase 4 (approved) | CDK2 |
| PACRITINIB | ChEMBL | Phase 4 (approved) | CDK2 |
| QUIZARTINIB | ChEMBL | Phase 4 (approved) | CDK2 |
| SORAFENIB | ChEMBL | Phase 4 (approved) | CDK2 |
| SUNITINIB | ChEMBL | Phase 4 (approved) | CDK4 |
| 6-O-BENZYLGUANINE | ChEMBL | Phase 3 | CDK2 |
| CRENOLANIB | ChEMBL | Phase 3 | CDK2 |
| DALPICICLIB | ChEMBL | Phase 3 | CDK4 |
| DEFACTINIB | ChEMBL | Phase 3 | CDK2 |
| DOVITINIB | ChEMBL | Phase 3 | CDK4 |
| ENZASTAURIN | ChEMBL | Phase 3 | CDK2 |
| INDIGO | ChEMBL | Phase 3 | CDK2 |
| RUBOXISTAURIN | ChEMBL | Phase 3 | CDK4 |
| SARACATINIB | ChEMBL | Phase 3 | CDK2 |
| ASNUCICLIB | ChEMBL | Phase 2 | CDK2 |
| AT-9283 | ChEMBL | Phase 2 | CDK4 |
| ATIRMOCICLIB | ChEMBL | Phase 2 | CDK4 |
| BI-2536 | ChEMBL | Phase 2 | CDK4 |
| BMS-754807 | ChEMBL | Phase 2 | CDK2 |
| BMS-919373 | ChEMBL | Phase 2 | CDK2 |
| CENISERTIB | ChEMBL | Phase 2 | CDK2 |
| CLOSANTEL | ChEMBL | Phase 2 | CDK2 |
| DANUSERTIB | ChEMBL | Phase 2 | CDK2 |
| ECIRUCICLIB | ChEMBL | Phase 2 | CDK4 |
| FISETIN | ChEMBL | Phase 2 | CDK2 |
| LAUROGUADINE | ChEMBL | Phase 2 | CDK2 |
| LUTEOLIN | ChEMBL | Phase 2 | CDK2 |
| R-406 | ChEMBL | Phase 2 | CDK2 |
| SALIRASIB | ChEMBL | Phase 2 | CDK2 |
| SILMITASERTIB | ChEMBL | Phase 2 | CDK2 |
| SIMUROSERTIB | ChEMBL | Phase 2 | CDK2 |
| SOTRASTAURIN | ChEMBL | Phase 2 | CDK2 |
| SU-014813 | ChEMBL | Phase 2 | CDK4 |
| UCN-01 | ChEMBL | Phase 2 | CDK2 |
| ZOTIRACICLIB | ChEMBL | Phase 2 | CDK2 |
| corydine | PubChem | Approved | CDK2 |
| Gefitinib | PubChem | Approved | CDK4 |
| Pomalidomide | PubChem | Approved | CDK4 |
Related Atlas pages
- Genes: CDK2, CDK4
- In clinical trials for: lymphoma, plasma cell myeloma, B-cell chronic lymphocytic leukemia, acute myeloid leukemia, cutaneous melanoma, sarcoma, prolymphocytic leukemia, kidney cancer, endometrium neoplasm, exocrine pancreatic carcinoma
- Drugs: Abemaciclib, Ceritinib, Dabrafenib, Gilteritinib, Nintedanib, Palbociclib, Ribociclib, Trilaciclib, Dinaciclib, Lerociclib, Lestaurtinib, Quercetin, Afatinib, Binimetinib, Crizotinib, dacomitinib, Fostamatinib, Idelalisib, Pazopanib, regorafenib, Selumetinib, Trametinib, Encorafenib, Erlotinib, Fedratinib, Lapatinib, Momelotinib, Pacritinib, Quizartinib, Sorafenib, Sunitinib, 6-O-BENZYLGUANINE, Crenolanib, Dalpiciclib, Defactinib, Dovitinib, Enzastaurin, Indigo, Ruboxistaurin, Saracatinib, Gefitinib, Pomalidomide
- Biomarker genes: CDKN2A