General Information of Drug (ID: DMSQZE2)

Drug Name
Asenapine Drug Info
Synonyms
Asenapi; Asenapine [INN:BAN]; Saphris (TN); [13C,2H3]-Asenipine; Trans-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz(2,3:6,7)oxepino(4,5-c)pyrrole; 1H-Dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, 5-chloro-2,3,3a,12b-tetrahydro-2-met; 5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz(2,3-6,7)oxepino(4,5-c)pyrrole
Indication
Disease Entry ICD 11 Status REF
Schizophrenia 6A20 Approved [1]
Cross-matching ID
PubChem CID
3036780
ChEBI ID
CHEBI:71246
CAS Number
CAS 65576-45-6
TTD Drug ID
DMSQZE2
INTEDE Drug ID
DR0146
ACDINA Drug ID
D00045

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Targeting Hyaluronidase (HYAL)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hyqvia DM0RXF5 Immunodeficiency 4A00-4A85 Approved [5]
PEGPH20 DM26YJ1 Non-small-cell lung cancer 2C25.Y Phase 2 [6]
PEGylated hyaluronidase (human recombinant) DM1D6BT Pancreatic cancer 2C10 Phase 1/2 [7]
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 [8]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [9]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [10]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [11]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [12]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [13]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [14]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [15]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [9]
Verapamil DMA7PEW Angina pectoris BA40 Approved [16]
⏷ 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 [17]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [18]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [19]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [20]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [21]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [22]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [14]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [23]
Verapamil DMA7PEW Angina pectoris BA40 Approved [24]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [25]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 2D6 (CYP2D6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [26]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [27]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [28]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [12]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [16]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [29]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [30]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [31]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [32]
Propranolol DM79NTF Angina pectoris BA40 Approved [33]
⏷ 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
Hyaluronidase (HYAL) TTXFI1K NOUNIPROTAC Modulator [2]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [3]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [4]
Cytochrome P450 1A2 (CYP1A2) Main DME DEJGDUW CP1A2_HUMAN Substrate [4]

References

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2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
3 Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504.
4 Asenapine review, part I: chemistry, receptor affinity profile, pharmacokinetics and metabolism. Expert Opin Drug Metab Toxicol. 2014 Jun;10(6):893-903.
5 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
6 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
7 Targeting the tumor microenvironment in cancer: why hyaluronidase deserves a second look. Cancer Discov. 2011 September; 1(4): 291-296.
8 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.
9 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
10 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.
11 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
12 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.
13 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.
14 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
15 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.
16 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.
17 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.
18 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.
19 Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1). Drug Metab Dispos. 2014 Nov;42(11):1843-50.
20 Cytochrome P450 1A2 (CYP1A2) activity and risk factors for breast cancer: a cross-sectional study. Breast Cancer Res. 2004;6(4):R352-65.
21 PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses. Pharmacogenet Genomics. 2015 Aug;25(8):416-26.
22 The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats. Biomed Res Int. 2013;2013:789184.
23 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.
24 Identification of P450 enzymes involved in metabolism of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1993 Sep;348(3):332-7.
25 Metabolism and metabolic inhibition of xanthotoxol in human liver microsomes. Evid Based Complement Alternat Med. 2016;2016:5416509.
26 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
27 Effect of genetic polymorphism on the metabolism of endogenous neuroactive substances, progesterone and p-tyramine, catalyzed by CYP2D6. Brain Res Mol Brain Res. 2004 Oct 22;129(1-2):117-23.
28 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
29 Inhibition of cytochrome P450 2D6: structure-activity studies using a series of quinidine and quinine analogues. Chem Res Toxicol. 2003 Apr;16(4):450-9.
30 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
31 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
32 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
33 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.