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Dalpiciclib

drug
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Also known as Shr-6390

Summary

Dalpiciclib (CHEMBL4802161) is a phase-3 clinical-stage small molecule targeting CDK4 and CDK6; indicated across 12 conditions including breast neoplasm and esophageal squamous cell carcinoma.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 2 (CDK4, CDK6)
  • Indications: 12 conditions
  • Clinical trials: 48
  • Chemistry: 446.5 Da · C25H30N6O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL4802161
NameDalpiciclib
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID86279927
Molecular formulaC25H30N6O2
Molecular weight446.5
InChIKeySGJLSPUSUBJWHO-UHFFFAOYSA-N

SMILES: CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)C4CCNCC4)C5CCCC5)C(=O)C

IUPAC name: 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperidin-4-yl-2-pyridinyl)amino]pyrido[2,3-d]pyrimidin-7-one

Also known as: Dalpiciclib, Shr-6390, DALPICICLIB

Patent coverage: 193 distinct patent families (423 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 396 (94%) 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).

GeneTargetActionpAffinityCancer dependencyUniProt
CDK4cyclin dependent kinase 4Inhibition7.9658%P11802
CDK6cyclin dependent kinase 6Inhibition8.2252.1%Q00534

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Cyclin-dependent kinase 6, Cyclin-dependent kinase 4.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
CDK68IC5010nMCHEMBL_ACT_29144582
CDK47.92IC5012nMCHEMBL_ACT_29144581

Target pathways

Aggregated over 2 target gene(s): CDK4, CDK6.

Top Reactome pathways

52 total, by targets touching each:

PathwayTargetsGenes
Cell Cycle2CDK4, CDK6
Disease2CDK4, CDK6
Generic Transcription Pathway2CDK4, CDK6
Cellular responses to stress2CDK4, CDK6
Oxidative Stress Induced Senescence2CDK4, CDK6
Senescence-Associated Secretory Phenotype (SASP)2CDK4, CDK6
Cellular Senescence2CDK4, CDK6
Oncogene Induced Senescence2CDK4, CDK6
Mitotic G1 phase and G1/S transition2CDK4, CDK6
Cyclin D associated events in G12CDK4, CDK6
G1 Phase2CDK4, CDK6
Cell Cycle, Mitotic2CDK4, CDK6
RNA Polymerase II Transcription2CDK4, CDK6
Gene expression (Transcription)2CDK4, CDK6
Cellular responses to stimuli2CDK4, CDK6
Diseases of Cellular Senescence2CDK4, CDK6
Evasion of Oncogene Induced Senescence Due to p16INK4A Defects2CDK4, CDK6
Evasion of Oncogene Induced Senescence Due to Defective p16INK4A binding to CDK4 and CDK62CDK4, CDK6
Evasion of Oxidative Stress Induced Senescence Due to p16INK4A Defects2CDK4, CDK6
Evasion of Oxidative Stress Induced Senescence Due to Defective p16INK4A binding to CDK4 and CDK62CDK4, CDK6
Aberrant regulation of mitotic G1/S transition in cancer due to RB1 defects2CDK4, CDK6
Defective binding of RB1 mutants to E2F1,(E2F2, E2F3)2CDK4, CDK6
Diseases of mitotic cell cycle2CDK4, CDK6
Diseases of cellular response to stress2CDK4, CDK6
Aberrant regulation of mitotic cell cycle due to RB1 defects2CDK4, CDK6
Drug-mediated inhibition of CDK4/CDK6 activity2CDK4, CDK6
Developmental Biology1CDK4
Reproduction1CDK4
Meiosis1CDK4
Signal Transduction1CDK4

Dominant GO biological processes

GO termTargets
G1/S transition of mitotic cell cycle2
signal transduction2
regulation of G2/M transition of mitotic cell cycle2
regulation of gene expression2
positive regulation of fibroblast proliferation2
cell division2
regulation of cell cycle2
protein phosphorylation2
positive regulation of cell population proliferation1
response to xenobiotic stimulus1
positive regulation of G2/M transition of mitotic cell cycle1
regulation of transcription initiation by RNA polymerase II1
regulation of type B pancreatic cell proliferation1
cellular response to lipopolysaccharide1
cellular response to interleukin-41

Indications & clinical

Indications

12 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).

IndicationTrial phaseMONDOEFO
breast neoplasm3MONDO:0021100EFO:0003869
esophageal squamous cell carcinoma2MONDO:0005580EFO:0005922
head and neck squamous cell carcinoma2MONDO:0010150EFO:0000181
neoplasm2MONDO:0005070EFO:0000616
exocrine pancreatic carcinoma2MONDO:0005192EFO:0002618
sarcoma2MONDO:0005089EFO:0000691
ovarian carcinoma2MONDO:0005140EFO:0001075
nasopharyngeal carcinoma2MONDO:0015459MONDO:0015459
melanoma1MONDO:0005105EFO:0000756
liver disorder1MONDO:0005154EFO:0001421
gastric neoplasm1MONDO:0021085MONDO:0001056

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 48.

Phase distribution

PhaseTrials
PHASE233
PHASE34
Not specified4
PHASE1/PHASE23
PHASE13
PHASE41

Top trials by phase / activity

NCTPhaseStatusTitle
NCT06613373PHASE4NOT_YET_RECRUITINGAn Exploratory Clinical Study of CDK4/6i Dalpiciclib Combined With AI Neoadjuvant Therapy for Stage II-III HR+/HER2- Breast Cancer
NCT06612814PHASE3ACTIVE_NOT_RECRUITINGPARP Inhibitor With CDK4/ 6 Inhibitor and Endocrine Therapy in HR+/ HER2-Advanced Breast Cancer
NCT07207070PHASE3RECRUITINGA Randomised, Open-label, Multicentre Phase III Clinical Study to Evaluate the Efficacy and Safety of JS105 Combined With Dalpiciclib and Fulvestrant Compared With Dalpiciclib and Fulvestrant in Patients With PIK3CA-mutated, HR-positive, HER2-negative Recurrent or Metastatic Breast Cancer.
NCT07432178PHASE3NOT_YET_RECRUITINGCDK4/6 Inhibitors Intensification for Chemotherapy Omission in Small Size High-risk ER-positive Breast Cancer（Cinnamon）
NCT07467330PHASE3RECRUITINGDalpiciclib Combined With Endocrine Therapy and Metronomic Capecitabine vs Dalpiciclib Combined With Endocrine Therapy for First-line Treatment
NCT05228951PHASE2RECRUITINGPyrotinib Maleate, Trastuzumab, SHR6390 and Letrozole in Combination for Stage II-III TPBC
NCT05463601PHASE2ACTIVE_NOT_RECRUITINGMecapegfilgrastim for the Prevention of Dalpiciclib -Induced Neutropenia in Advanced Breast Cancer
NCT05582499PHASE2RECRUITINGFudan University Shanghai Cancer Center Breast Cancer Precision Platform Series Study- Neoadjuvant Therapy
NCT05594095PHASE2RECRUITINGSNF Platform Study of HR+/ HER2-advanced Breast Cancer
NCT05638594PHASE2RECRUITINGPyrotinib Combined With Trastuzumab, Dalpiciclib, Letrozole Versus TCbHP (Trastuzumab Plus Pertuzumab With Docetaxel and Carboplatin) as Neoadjuvant Treatment in HR +/HER2 + Breast Cancer
NCT05759546PHASE2RECRUITINGPARP Inhibitor With CDK4/6 Inhibitor and Endocrine Therapy in HR+/ HER2-Advanced Breast Cancer
NCT05759572PHASE2RECRUITINGApatinib With CDK4/6 Inhibitor and Endocrine Therapy in HR+/ HER2- Advanced Breast Cancer
NCT06107673PHASE2RECRUITINGDalpiciclib Plus AI (Neoadjuvant Endocrine Therapy) Compared With Neoadjuvant Chemotherapy in Early Breast Cancer （EBC）
NCT06149130PHASE2RECRUITINGAdebrelimab Combined With Dalpiciclib and Standard Endocrine Therapy for HR+/HER2 - Advanced Breast Cancer
NCT06199271PHASE2NOT_YET_RECRUITINGNeoadjuvant Adebrelimab Plus Dalpiciclib in Head and Neck Squamous Cell Carcinoma
NCT06208410PHASE1/PHASE2RECRUITINGA Clinical Study of JS105 in Combination With Other Anti-tumor Therapies in Patients With Solid Tumors
NCT06341894PHASE2RECRUITINGEfficacy and Safety of Dalpiciclib With Endocrine Therapy as Adjuvant Treatment in HR+/ HER2- Early Breast Cancer
NCT06552858PHASE2NOT_YET_RECRUITINGFluzoparib Combined With Dalpiciclib for Platinum Resistant Recurrent Ovarian Cancer
NCT06556862PHASE2NOT_YET_RECRUITINGExploration of Dalpiciclib Plus HDACi in HR+/HER2- Advanced Breast Cancer After Failure of CDK4/6 Inhibitor
NCT06650748PHASE2ENROLLING_BY_INVITATIONMultigene Risk Score Combined With Ki-67 Dynamic Assessment in Stratified Neoadjuvant Endocrine Therapy Treatment With or Without CDK4/6 Inhibitors in HR+/HER2- Breast Cancer
NCT06684600PHASE2RECRUITINGStudy of Dalpiciclib Isethionate Plus Pyrotinib Maleate in the Treatment of Advanced Esophageal Squamous Cell Carcinoma
NCT06970912PHASE2RECRUITINGctDNA-Guided De-Escalation of Adjuvant Chemotherapy With Dalpiciclib in HR-Positive/HER2-Negative Breast Cancer
NCT07101159PHASE2NOT_YET_RECRUITINGDalpiciclib as Adjuvant Therapy for HR-positive/HER2-negative Early-stage Patients
NCT07179939PHASE2NOT_YET_RECRUITINGMaintenance Therapy in HER2-Positive Unresectable Locally Recurrent or Metastatic Breast Cancer: A Phase II Study
NCT07238881PHASE2RECRUITINGDalpiciclib Plus Camrelizumab for HCC Patients Who Have Previously Received ICI Treatment
NCT07285382PHASE2RECRUITINGDifferent Doses of Dalpicicl Combined With Letrozole in the First-line Treatment of HR-positive, HER2-negative Advanced Breast Cancer
NCT07492394PHASE2RECRUITINGDalpiciclib With or Without Entinostat and Letrozole in HR+/HER2- Early Breast Cancer
NCT07539753PHASE2NOT_YET_RECRUITINGBrain Radiotherapy Combined With Dalpiciclib and Endocrine Therapy in HR-Positive/HER2-Negative Advanced Breast Cancer With Brain Metastases
NCT07581834PHASE2RECRUITINGEfficacy and Safety of Dalpiciclib Combined With Endocrine Adjuvant Therapy for Early HR +/HER2- Breast Cancer: a Multicenter, Prospective Clinical Study
NCT07610720PHASE2RECRUITINGDalpiciclib, Anti-HER2 Therapy, and Endocrine Therapy for Hormone-Receptor-Positive, HER2-Positive Metastatic Breast Cancer
NCT03772353PHASE1/PHASE2UNKNOWNPyrotinib, Dalpiciclib(SHR6390) and Endocrine Therapy in Subjects With Dual-receptor Positive(ER+/HER2+) Advanced Breast Cancer
NCT04866381PHASE2UNKNOWNAn Exploratory Clinical Study of SHR6390 and SHR1020 in the Treatment of Esophageal Squamous Cell Carcinoma After Progression on PD-1 Antibody
NCT05328440PHASE2UNKNOWNTreatment of Dalpiciclib Combined With Pyrotinib for Trastuzumab-sensitive HER2+ Advanced Breast Cancer(DAP-Her-02)
NCT05469750PHASE2UNKNOWNDalpiciclib Plus Letrozole and Capecitabine
NCT05480280PHASE2UNKNOWNmFOLFOX6 Combined With Dalpiciclib in Patients With Metastatic Colorectal Cancer
NCT05512780PHASE2UNKNOWNDalpiciclib Combined With Letrozole in Neoadjuvant Treatment of Stage Ⅱ-Ⅲ HR-positive/HER2-negative Breast Cancer
NCT05574881PHASE1/PHASE2UNKNOWNDalpiciclib, Fulvestrant, Trastuzumab and Pertuzumab in HR Positive, HER2 Positive Metastatic Breast Cancer
NCT05577923PHASE2UNKNOWNExploring Whether Disease-free Intervals Can Guide Endocrine Combined Targeted Therapy for ER+/HER2+ Advanced Breast Cancer (T-sunflower)
NCT05721443PHASE2UNKNOWNCetuximab Plus Dalpicilib in Patients With HPV Negative, PD-1 Resistant R/M HNSCC
NCT05806671PHASE2UNKNOWNDalpiciclib Plus Fulvestrant With Pyrotinib in Hormone Receptor-positive, HER2-low Advanced Breast Cancer That Progressed on Previous CDK4/6i Plus AI Therapy

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.

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.

63 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
ABEMACICLIBChEMBLPhase 4 (approved)CDK4, CDK6
DABRAFENIBChEMBLPhase 4 (approved)CDK4, CDK6
PALBOCICLIBChEMBLPhase 4 (approved)CDK4, CDK6
RIBOCICLIBChEMBLPhase 4 (approved)CDK4, CDK6
TRILACICLIBChEMBLPhase 4 (approved)CDK4, CDK6
ALVOCIDIBChEMBLPhase 3CDK4, CDK6
DINACICLIBChEMBLPhase 3CDK4, CDK6
DOVITINIBChEMBLPhase 3CDK4, CDK6
LEROCICLIBChEMBLPhase 3CDK4, CDK6
LESTAURTINIBChEMBLPhase 3CDK4, CDK6
QUERCETINChEMBLPhase 3CDK4, CDK6
AT-7519ChEMBLPhase 2CDK4, CDK6
AT-9283ChEMBLPhase 2CDK4, CDK6
ATIRMOCICLIBChEMBLPhase 2CDK4, CDK6
CROZBACICLIBChEMBLPhase 2CDK4, CDK6
CT-7001ChEMBLPhase 2CDK4, CDK6
CULMERCICLIBChEMBLPhase 2CDK4, CDK6
EBVACICLIBChEMBLPhase 2CDK4, CDK6
ECIRUCICLIBChEMBLPhase 2CDK4, CDK6
INDIRUBINChEMBLPhase 2CDK4, CDK6
INIXACICLIBChEMBLPhase 2CDK4, CDK6
ISTISOCICLIBChEMBLPhase 2CDK4, CDK6
MILCICLIBChEMBLPhase 2CDK4, CDK6
NARAZACICLIBChEMBLPhase 2CDK4, CDK6
RG-547ChEMBLPhase 2CDK4, CDK6
RIVICICLIBChEMBLPhase 2CDK4, CDK6
SELICICLIBChEMBLPhase 2CDK4, CDK6
TEGTOCICLIBChEMBLPhase 2CDK4, CDK6
ULECACICLIBChEMBLPhase 2CDK4, CDK6
VORUCICLIBChEMBLPhase 2CDK4, CDK6
ZEMIRCICLIBChEMBLPhase 2CDK4, CDK6
AfatinibPubChemApprovedCDK4, CDK6
BinimetinibPubChemApprovedCDK4, CDK6
CrizotinibPubChemApprovedCDK4, CDK6
dacomitinibPubChemApprovedCDK4, CDK6
FostamatinibPubChemApprovedCDK4, CDK6
GefitinibPubChemApprovedCDK4, CDK6
IdelalisibPubChemApprovedCDK4, CDK6
PazopanibPubChemApprovedCDK4, CDK6
PomalidomidePubChemApprovedCDK4, CDK6
regorafenibPubChemApprovedCDK4, CDK6
SelumetinibPubChemApprovedCDK4, CDK6
TrametinibPubChemApprovedCDK4, CDK6
CERITINIBChEMBLPhase 4 (approved)CDK4
ENCORAFENIBChEMBLPhase 4 (approved)CDK4
FEDRATINIBChEMBLPhase 4 (approved)CDK4
GILTERITINIBChEMBLPhase 4 (approved)CDK4
MOMELOTINIBChEMBLPhase 4 (approved)CDK6
NINTEDANIBChEMBLPhase 4 (approved)CDK4
OLAPARIBChEMBLPhase 4 (approved)CDK6
SORAFENIBChEMBLPhase 4 (approved)CDK6
SUNITINIBChEMBLPhase 4 (approved)CDK4
RUBOXISTAURINChEMBLPhase 3CDK4
BI-2536ChEMBLPhase 2CDK4
CYC-065ChEMBLPhase 2CDK4
ELLAGIC ACIDChEMBLPhase 2CDK4
FISETINChEMBLPhase 2CDK6
LY-2090314ChEMBLPhase 2CDK4
REBASTINIBChEMBLPhase 2CDK4
RONICICLIBChEMBLPhase 2CDK4

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot