General Information of Drug (ID: DMZFIGQ)

Drug Name
TG02 Drug Info
Synonyms
SB1317; 937270-47-8; TG02; TG-02; TG02 (Double bond Z/E); UNII-40D08182TT; CHEMBL1944698; 40D08182TT; SB-1317; 1204918-72-8; C23H24N4O; Tube011; SB-1317 free base; TG02 (Double bond E); TG02 [WHO-DD]; SCHEMBL823947; SCHEMBL2298965; GTPL9095; SCHEMBL17595943; EX-A239; MolPort-039-139-793; AOB87361; BCP07033; ZINC68251500; BDBM50363196; 4029AH; AKOS030527020; AKOS032950000; SB1317(TG-02); SB14606; CS-0884; compound 26h [PMID: 22148278]; KB-80503; HY-15166; W-5884
Indication
Disease Entry ICD 11 Status REF
Anaplastic astrocytoma 2A00.0 Phase 1/2 [1]
Recurrent glioblastoma 2A00.00 Phase 1/2 [1]
Solid tumour/cancer 2A00-2F9Z Phase 1 [2]
Cross-matching ID
PubChem CID
16739650
CAS Number
CAS 1204918-72-8
TTD Drug ID
DMZFIGQ
INTEDE Drug ID
DR1818

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
Drug Status:
Clinical Trial Drug(s)
Patented Agent(s)
Investigative Drug(s)
Discontinued Drug(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 [5]
Ro 31-7453 DM83QCL Solid tumour/cancer 2A00-2F9Z Phase 2 [6]
PHA848125 DMS2Q9G Thymic cancer 2C27 Phase 2 [7]
NUV-422 DMQJQNT Malignant glioma 2A00.0 Phase 1/2 [8]
RGB-286638 DMEGOQP Haematological malignancy 2B33.Y Phase 1 [9]
FN-1501 DM7BMD6 Solid tumour/cancer 2A00-2F9Z Phase 1 [10]
AG-024322 DMY4WVK Solid tumour/cancer 2A00-2F9Z Phase 1 [5]
PHA-793887 DM2Y4FG Solid tumour/cancer 2A00-2F9Z Phase 1 [11]
SNS-032 DMEITAS Solid tumour/cancer 2A00-2F9Z Phase 1 [12]
CYC065 DM9ODT6 Lymphoma 2A80-2A86 Phase 1 [1]
⏷ 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 [13]
Flavopiridol DMKSUOI Acute myeloid leukaemia 2A60 Phase 2 [14]
PF-06873600 DMRZHV6 Breast cancer 2C60-2C65 Phase 1 [1]
PMID26161698-Compound-44 DM8UPO3 N. A. N. A. Patented [15]
Purine derivative 4 DMYD5SQ N. A. N. A. Patented [15]
Indole-based analog 12 DM1CNRH N. A. N. A. Patented [15]
PMID26161698-Compound-10 DMXVCHZ N. A. N. A. Patented [15]
BS-194 DMLXFHD Solid tumour/cancer 2A00-2F9Z Investigative [16]
⏷ Show the Full List of 8 Drug(s)
Drug(s) Targeting Protein kinase (PK)
Drug Name Drug ID Indication ICD 11 Highest Status REF
MGCD516 DM752PU Solid tumour/cancer 2A00-2F9Z Phase 2/3 [1]
LY2801653 DM0KJDY Biliary tract cancer 2C17 Phase 2 [1]
MGCD265 DMRPCF2 Non-small-cell lung cancer 2C25.Y Phase 2 [1]
ENMD-2076 DMJZVPB Acute myeloid leukaemia 2A60 Phase 2 [1]
RV-568 DM652CM Asthma CA23 Phase 2 [17]
LX-7101 DM2LYIN Glaucoma/ocular hypertension 9C61 Phase 1/2 [18]
Cyclocreatine DM1I7UO Virus infection 1A24-1D9Z Discontinued in Phase 1 [19]
⏷ Show the Full List of 7 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [20]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [21]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [22]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [23]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [24]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [25]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [26]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [27]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [21]
Verapamil DMA7PEW Angina pectoris BA40 Approved [28]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 1A2 (CYP1A2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [29]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [30]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [31]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [32]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [33]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [34]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [26]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [35]
Verapamil DMA7PEW Angina pectoris BA40 Approved [36]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [37]
⏷ 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 (CDK) TTMBO1Z NOUNIPROTAC Inhibitor [1]
Cyclin-dependent kinase 2 (CDK2) TT7HF4W CDK2_HUMAN Modulator [2]
Protein kinase (PK) TTU8W4S NOUNIPROTAC Inhibitor [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [4]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Substrate [4]

References

1 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2 Preclinical metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor. Drug Metab Lett. 2012 Mar;6(1):33-42.
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 Preclinical metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor. Drug Metab Lett. 2012 Mar;6(1):33-42.
5 Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
6 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.
7 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.
8 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.
9 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.
10 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.
11 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.
12 Mechanism of action of SNS-032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia. Blood. 2009 May 7;113(19):4637-45.
13 Therapeutic efficacy of seliciclib in combination with ionizing radiation for human nasopharyngeal carcinoma.Clin Cancer Res. 2009 Jun 1;15(11):3716-24.
14 Pharma & Vaccines. Product Development Pipeline. April 29 2009.
15 Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 - 2014).Expert Opin Ther Pat. 2015;25(9):953-70.
16 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: 8176).
17 Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary disease. Expert Opin Investig Drugs. 2015 Mar;24(3):383-92.
18 Design, synthesis and biological characterization of selective LIMK inhibitors. Bioorg Med Chem Lett. 2015 Sep 15;25(18):4005-10.
19 Direct determination of creatine kinase equilibrium constants with creatine or cyclocreatine substrate. Biochim Biophys Acta. 1989 Oct 19;998(3):317-20.
20 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
21 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
22 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
23 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
24 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
25 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
26 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
27 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
28 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
29 Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
30 Effects of polyunsaturated fatty acids on prostaglandin synthesis and cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines in human adenocarcinoma colon cells. Mol Carcinog. 2004 Jul;40(3):180-8.
31 Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1). Drug Metab Dispos. 2014 Nov;42(11):1843-50.
32 Cytochrome P450 1A2 (CYP1A2) activity and risk factors for breast cancer: a cross-sectional study. Breast Cancer Res. 2004;6(4):R352-65.
33 PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses. Pharmacogenet Genomics. 2015 Aug;25(8):416-26.
34 The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats. Biomed Res Int. 2013;2013:789184.
35 The influence of metabolic gene polymorphisms on urinary 1-hydroxypyrene concentrations in Chinese coke oven workers. Sci Total Environ. 2007 Aug 1;381(1-3):38-46.
36 Identification of P450 enzymes involved in metabolism of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1993 Sep;348(3):332-7.
37 Metabolism and metabolic inhibition of xanthotoxol in human liver microsomes. Evid Based Complement Alternat Med. 2016;2016:5416509.