General Information of Drug (ID: DM2Y4FG)

Drug Name
PHA-793887 Drug Info
Synonyms Cyclin-dependent kinase inhibitor (cancer), Nerviano
Indication
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Phase 1 [1]
Cross-matching ID
PubChem CID
46191454
ChEBI ID
CHEBI:91371
CAS Number
CAS 718630-59-2
TTD Drug ID
DM2Y4FG

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Patented Agent(s)
Approved Drug(s)
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]
P276-00 DM9DJL2 Mantle cell lymphoma 2A85.5 Phase 2 [3]
P-276 DMMJUHD Breast cancer 2C60-2C65 Phase 2 [5]
RGB-286638 DMEGOQP Haematological malignancy 2B33.Y Phase 1 [6]
AG-024322 DMY4WVK Solid tumour/cancer 2A00-2F9Z Phase 1 [3]
Oxazolyl methylthiothiazole derivative 1 DMZM6FW N. A. N. A. Patented [7]
PMID25991433-Compound-A1 DM89LF0 N. A. N. A. Patented [8]
KENPAULLONE DMAGVXW Discovery agent N.A. Patented [9]
Roscovitine derivative 1 DMD1G3Z N. A. N. A. Patented [7]
⏷ Show the Full List of 10 Drug(s)
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 [10]
TG02 DMZFIGQ Anaplastic astrocytoma 2A00.0 Phase 1/2 [11]
NUV-422 DMQJQNT Malignant glioma 2A00.0 Phase 1/2 [12]
RGB-286638 DMEGOQP Haematological malignancy 2B33.Y Phase 1 [6]
FN-1501 DM7BMD6 Solid tumour/cancer 2A00-2F9Z Phase 1 [13]
AG-024322 DMY4WVK Solid tumour/cancer 2A00-2F9Z Phase 1 [3]
SNS-032 DMEITAS Solid tumour/cancer 2A00-2F9Z Phase 1 [14]
CYC065 DM9ODT6 Lymphoma 2A80-2A86 Phase 1 [15]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Apremilast DMTWS9E Psoriasis vulgaris EA90 Approved [16]
LY2835219 DM93VBZ Breast cancer 2C60-2C65 Approved [17]
Palbociclib DMD7L94 Breast cancer 2C60-2C65 Approved [18]
Ribociclib Succinate DM9CIUW Breast cancer 2C60-2C65 Approved [19]
Trilaciclib DMP5A4T Small-cell lung cancer 2C25.Y Approved [20]
LEE011 DMMX75K Breast cancer 2C60-2C65 Phase 3 [21]
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 [2]
G1T38 DMQO2IT Breast cancer 2C60-2C65 Phase 2 [15]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Cyclin-dependent kinase 1 (CDK1) TTH6V3D CDK1_HUMAN Inhibitor [1]
Cyclin-dependent kinase 2 (CDK2) TT7HF4W CDK2_HUMAN Inhibitor [1]
Cyclin-dependent kinase 4 (CDK4) TT0PG8F CDK4_HUMAN Inhibitor [2]

References

1 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.
2 Liposarcoma: molecular genetics and therapeutics. Sarcoma. 2011;2011:483154.
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 P276-00, a novel cyclin-dependent inhibitor induces G1-G2 arrest, shows antitumor activity on cisplatin-resistant cells and significant in vivo efficacy in tumor models. Mol Cancer Ther. 2007 Mar;6(3):926-34.
6 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.
7 Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 - 2014).Expert Opin Ther Pat. 2015;25(9):953-70.
8 c-Jun N-terminal kinase inhibitors: a patent review (2010 - 2014).Expert Opin Ther Pat. 2015;25(8):849-72.
9 Discovery of novel CDK1 inhibitors by combining pharmacophore modeling, QSAR analysis and in silico screening followed by in vitro bioassay. Eur J Med Chem. 2010 Sep;45(9):4316-30.
10 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.
11 Preclinical metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor. Drug Metab Lett. 2012 Mar;6(1):33-42.
12 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.
13 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.
14 Mechanism of action of SNS-032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia. Blood. 2009 May 7;113(19):4637-45.
15 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
16 Agreement signed with Prostagenics to develop prostate cancer treatment. Innovate Oncology, Inc. 2005.
17 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
18 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2017
19 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
20 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
21 Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82.