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

General Information of Drug (ID: DM7BMD6)

• Drug Name: FN-1501 Drug Info
• Synonyms: 1429515-59-2; CHEMBL4077071; UNII-6MC966B505; TQR1001; BDBM50270304; NSC781143; 6MC966B505; NSC-781143; HY-111361; CS-0039834; 4((7HPyrrolo[2,3d]pyrimidin-4-yl)amino)N(4-((4-methylpiperazin-1-yl)methyl)phenyl)1Hpyrazole-3-carboxamide; 4-((7H-Pyrrolo (2,3-d)pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide; 4-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-5-carboxamide; 4a?(7Ha'Pyrrolo[2,3a'd]pyrimidin-4-yl)amino)a'Na?4-((4-methylpiperazin-1-yl)methyl)phenyl)a?Ha'pyrazole-3-carboxamide; N-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-4-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1H-pyrazole-5-carboxamide

Indication

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

• Cross-matching ID:
  PubChem CID: 72195175
  CAS Number: CAS 1429515-59-2
  TTD Drug ID: DM7BMD6

Molecule-Related Drug Atlas

Drug(s) Targeting Cyclin-dependent kinase 2 (CDK2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
R-roscovitine	DMSH108	Non-small-cell lung cancer	2C25.Y	Phase 2	[3]
Ro 31-7453	DM83QCL	Solid tumour/cancer	2A00-2F9Z	Phase 2	[4]
PHA848125	DMS2Q9G	Thymic cancer	2C27	Phase 2	[5]
TG02	DMZFIGQ	Anaplastic astrocytoma	2A00.0	Phase 1/2	[6]
NUV-422	DMQJQNT	Malignant glioma	2A00.0	Phase 1/2	[7]
RGB-286638	DMEGOQP	Haematological malignancy	2B33.Y	Phase 1	[8]
AG-024322	DMY4WVK	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
PHA-793887	DM2Y4FG	Solid tumour/cancer	2A00-2F9Z	Phase 1	[9]
SNS-032	DMEITAS	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]
CYC065	DM9ODT6	Lymphoma	2A80-2A86	Phase 1	[11]

Drug(s) Targeting Fms-like tyrosine kinase 3 (FLT-3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[12]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[13]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[14]
Midostaurin	DMI6E0R	Acute myeloid leukaemia	2A60	Approved	[4]
Gilteritinib	DMTI0ZO	Acute myeloid leukaemia	2A60	Approved	[15]
Pexidartinib	DMS2J0Z	Tenosynovial giant cell tumour	2F7B	Approved	[16]
Pacritinib	DM1T6ZN	Myelofibrosis	2A20.2	Approved	[12]
Quizartinib	DM8Y4JS	Acute myeloid leukaemia	2A60	Approved	[11]
Lestaurtinib	DMQ2AIJ	Acute myeloid leukaemia	2A60	Approved (orphan drug)	[17]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[18]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Apremilast	DMTWS9E	Psoriasis vulgaris	EA90	Approved	[19]
LY2835219	DM93VBZ	Breast cancer	2C60-2C65	Approved	[20]
Palbociclib	DMD7L94	Breast cancer	2C60-2C65	Approved	[21]
Ribociclib Succinate	DM9CIUW	Breast cancer	2C60-2C65	Approved	[22]
Trilaciclib	DMP5A4T	Small-cell lung cancer	2C25.Y	Approved	[23]
LEE011	DMMX75K	Breast cancer	2C60-2C65	Phase 3	[24]
Ro 31-7453	DM83QCL	Solid tumour/cancer	2A00-2F9Z	Phase 2	[4]
P276-00	DM9DJL2	Mantle cell lymphoma	2A85.5	Phase 2	[3]
P-276	DMMJUHD	Breast cancer	2C60-2C65	Phase 2	[25]
G1T38	DMQO2IT	Breast cancer	2C60-2C65	Phase 2	[11]

Drug(s) Targeting Cyclin-dependent kinase 6 (CDK6)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Apremilast	DMTWS9E	Psoriasis vulgaris	EA90	Approved	[19]
LY2835219	DM93VBZ	Breast cancer	2C60-2C65	Approved	[20]
Palbociclib	DMD7L94	Breast cancer	2C60-2C65	Approved	[21]
Ribociclib Succinate	DM9CIUW	Breast cancer	2C60-2C65	Approved	[22]
Trilaciclib	DMP5A4T	Small-cell lung cancer	2C25.Y	Approved	[23]
LEE011	DMMX75K	Breast cancer	2C60-2C65	Phase 3	[24]
G1T38	DMQO2IT	Breast cancer	2C60-2C65	Phase 2	[11]
GLR2007	DM7DWLY	Glioblastoma of brain	2A00.00	Phase 1/2	[26]
FCN-437	DMQ8VUW	Breast cancer	2C60-2C65	Phase 1/2	[27]
NUV-422	DMQJQNT	Malignant glioma	2A00.0	Phase 1/2	[7]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Cyclin-dependent kinase 2 (CDK2)	TT7HF4W	CDK2_HUMAN	Inhibitor	[2]
Cyclin-dependent kinase 4 (CDK4)	TT0PG8F	CDK4_HUMAN	Inhibitor	[2]
Cyclin-dependent kinase 6 (CDK6)	TTO0FDJ	CDK6_HUMAN	Inhibitor	[2]
Fms-like tyrosine kinase 3 (FLT-3)	TTGJCWZ	FLT3_HUMAN	Inhibitor	[2]

References

• [1] ClinicalTrials.gov (NCT03690154) A Phase 1 Study to Evaluate FN-1501 Monotherapy in Patients With Advanced Solid Tumors and R/R AML. U.S. National Institutes of Health.
• [2] 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.
• [3] Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
• [4] 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.
• [5] Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor. J Med Chem. 2009 Aug 27;52(16):5152-63.
• [6] Preclinical metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor. Drug Metab Lett. 2012 Mar;6(1):33-42.
• [7] 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.
• [8] Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. Leukemia. 2013 Dec;27(12):2366-75.
• [9] A first in man, phase I dose-escalation study of PHA-793887, an inhibitor of multiple cyclin-dependent kinases (CDK2, 1 and 4) reveals unexpected h... Cell Cycle. 2011 Mar 15;10(6):963-70.
• [10] Mechanism of action of SNS-032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia. Blood. 2009 May 7;113(19):4637-45.
• [11] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [12] 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. (Target id: 1807).
• [13] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [14] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [15] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [16] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [17] Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with ... Blood. 2008 Jun 15;111(12):5663-71.
• [18] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [19] Agreement signed with Prostagenics to develop prostate cancer treatment. Innovate Oncology, Inc. 2005.
• [20] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [21] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2017
• [22] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [23] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
• [24] Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82.
• [25] Liposarcoma: molecular genetics and therapeutics. Sarcoma. 2011;2011:483154.
• [26] Clinical pipeline report, company report or official report of Gan & Lee Pharmaceuticals.
• [27] Clinical pipeline report, company report or official report of Fochon Pharmaceuticals.