Drug General Information
Drug ID	D08MXP
Former ID	DIB001419
Drug Name	LEE011
Drug Type	Small molecular drug
Indication	Cancer [ICD9: 140-229; ICD10:C00-C96]		Phase 3	[524461], [542405]
Company	Novartis AG
Structure		Download 2D MOL 3D MOL
Formula	C23H30N8O
InChIKey	RHXHGRAEPCAFML-UHFFFAOYSA-N
PubChem Compound ID	44631912
PubChem Substance ID	87793394, 120110003, 138555830, 140717308, 175444442, 178103955, 196411464, 198983029, 198993418, 210275346, 210280994, 223370367, 223404354, 223405967, 224379035, 226642892, 247056333, 249814497, 252148259, 252160882, 252215684, 252451787, 252472287, 252543483
Target and Pathway
Target(s)	Cell division protein kinase 4	Target Info	Modulator	[532480]
	Cell division protein kinase 6	Target Info	Modulator	[532480]
KEGG Pathway	Cell cycle
	p53 signaling pathway
	PI3K-Akt signaling pathway
	Tight junction
	T cell receptor signaling pathway
	Hepatitis B
	Measles
	HTLV-I infection
	Pathways in cancer
	Viral carcinogenesis
	Pancreatic cancer
	Glioma
	Melanoma
	Bladder cancer
	Chronic myeloid leukemia
	Small cell lung cancer
	Non-small cell lung cancerhsa04110:Cell cycle
	MicroRNAs in cancer
	Non-small cell lung cancer
NetPath Pathway	TCR Signaling Pathway
	EGFR1 Signaling Pathway
	RANKL Signaling PathwayNetPath_7:TGF_beta_Receptor Signaling Pathway
Pathway Interaction Database	Regulation of nuclear SMAD2/3 signaling
	Calcineurin-regulated NFAT-dependent transcription in lymphocytes
	Validated targets of C-MYC transcriptional activation
	ATF-2 transcription factor network
	FOXM1 transcription factor network
	Regulation of retinoblastoma proteinp73pathway:p73 transcription factor network
	Coregulation of Androgen receptor activity
	C-MYB transcription factor network
	IL2 signaling events mediated by STAT5
	Regulation of retinoblastoma protein
Reactome	Oxidative Stress Induced Senescence
	Senescence-Associated Secretory Phenotype (SASP)
	Oncogene Induced Senescence
	RMTs methylate histone arginines
	Transcriptional regulation of white adipocyte differentiation
	Ubiquitin-dependent degradation of Cyclin D1
	Cyclin D associated events in G1
	Meiotic recombinationR-HSA-2559580:Oxidative Stress Induced Senescence
WikiPathways	DNA Damage Response
	G1 to S cell cycle control
	Ovarian Infertility Genes
	PPAR Alpha Pathway
	Bladder Cancer
	S Phase
	Transcriptional Regulation of White Adipocyte Differentiation
	Meiotic Recombination
	Retinoblastoma (RB) in Cancer
	Spinal Cord Injury
	Integrated Pancreatic Cancer Pathway
	Prostate Cancer
	Signaling Pathways in Glioblastoma
	TSH signaling pathway
	Integrated Breast Cancer Pathway
	Integrated Cancer pathway
	Mitotic G1-G1/S phases
	Cell Cycle
	miRNA Regulation of DNA Damage ResponseWP707:DNA Damage Response
	Wnt Signaling Pathway Netpath
	Metastatic brain tumor
	miR-targeted genes in muscle cell - TarBase
	miR-targeted genes in lymphocytes - TarBase
	miR-targeted genes in leukocytes - TarBase
	miR-targeted genes in epithelium - TarBase
	miRNAs involved in DNA damage response
	miRNA Regulation of DNA Damage Response
References
Ref 524461	ClinicalTrials.gov (NCT01958021) Study of Efficacy and Safety of LEE011 in Postmenopausal Women With Advanced Breast Cancer.(MONALEESA-2). U.S. National Institutes of Health.
Ref 542405	(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7383).
Ref 532480	Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82.

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