Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMMX75K)

Drug Name

LEE011 Drug Info

Synonyms

Ribociclib; LEE011; 1211441-98-3; LEE-011; Kisqali; Ribociclib(LEE011); UNII-TK8ERE8P56; LEE 011; 7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide; TK8ERE8P56; Ribociclib (LEE011); AK174906; 7-cyclopentyl-N,N-dimethyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide; 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo [2,3-d]pyrimidine-6-carboxylic acid dimethylamide; Ribociclib [USAN:INN]; LEE011A; Tube013

Indication

Disease Entry	ICD 11	Status	REF
Breast cancer	2C60-2C65	Phase 3	[1]
Solid tumour/cancer	2A00-2F9Z	Phase 3	[2]

Cross-matching ID

PubChem CID: 44631912
ChEBI ID: CHEMBL3545110
CAS Number: CAS 1211441-98-3
TTD Drug ID: DMMX75K

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

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Drug(s) Targeting Cyclin-dependent kinase 4 (CDK4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Apremilast	DMTWS9E	Psoriasis vulgaris	EA90	Approved	[4]
LY2835219	DM93VBZ	Breast cancer	2C60-2C65	Approved	[5]
Palbociclib	DMD7L94	Breast cancer	2C60-2C65	Approved	[6]
Ribociclib Succinate	DM9CIUW	Breast cancer	2C60-2C65	Approved	[7]
Trilaciclib	DMP5A4T	Small-cell lung cancer	2C25.Y	Approved	[8]
Ro 31-7453	DM83QCL	Solid tumour/cancer	2A00-2F9Z	Phase 2	[9]
P276-00	DM9DJL2	Mantle cell lymphoma	2A85.5	Phase 2	[10]
P-276	DMMJUHD	Breast cancer	2C60-2C65	Phase 2	[11]
G1T38	DMQO2IT	Breast cancer	2C60-2C65	Phase 2	[1]
GLR2007	DM7DWLY	Glioblastoma of brain	2A00.00	Phase 1/2	[12]
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Drug(s) Targeting Cyclin-dependent kinase 6 (CDK6)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Apremilast	DMTWS9E	Psoriasis vulgaris	EA90	Approved	[4]
LY2835219	DM93VBZ	Breast cancer	2C60-2C65	Approved	[5]
Palbociclib	DMD7L94	Breast cancer	2C60-2C65	Approved	[6]
Ribociclib Succinate	DM9CIUW	Breast cancer	2C60-2C65	Approved	[7]
Trilaciclib	DMP5A4T	Small-cell lung cancer	2C25.Y	Approved	[8]
G1T38	DMQO2IT	Breast cancer	2C60-2C65	Phase 2	[1]
GLR2007	DM7DWLY	Glioblastoma of brain	2A00.00	Phase 1/2	[12]
FCN-437	DMQ8VUW	Breast cancer	2C60-2C65	Phase 1/2	[13]
NUV-422	DMQJQNT	Malignant glioma	2A00.0	Phase 1/2	[14]
FN-1501	DM7BMD6	Solid tumour/cancer	2A00-2F9Z	Phase 1	[15]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Cyclin-dependent kinase 4 (CDK4)	TT0PG8F	CDK4_HUMAN	Modulator	[3]
Cyclin-dependent kinase 6 (CDK6)	TTO0FDJ	CDK6_HUMAN	Modulator	[3]

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References

1	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2	URL: 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).
3	Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82.
4	Agreement signed with Prostagenics to develop prostate cancer treatment. Innovate Oncology, Inc. 2005.
5	Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
6	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2017
7	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
8	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
9	A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
10	Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
11	Liposarcoma: molecular genetics and therapeutics. Sarcoma. 2011;2011:483154.
12	Clinical pipeline report, company report or official report of Gan & Lee Pharmaceuticals.
13	Clinical pipeline report, company report or official report of Fochon Pharmaceuticals.
14	ClinicalTrials.gov (NCT04541225) Phase 1/2 Dose Escalation, Safety, Pharmacokinetics, and Efficacy Study of NUV-422 in Adults With Recurrent or Refractory High-grade Gliomas and Solid Tumors. U.S.National Institutes of Health.
15	Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia. J Med Chem. 2018 Feb 22;61(4):1499-1518.