General Information of the Drug (ID: M6APDG03331)
Name
Glasdegib
Synonyms
Glasdegib; 1095173-27-5; PF 04449913; UNII-K673DMO5H9; K673DMO5H9; CHEMBL2043437; Glasdegib (PF-04449913); Glasdegib [USAN:INN]; Glasdegib (USAN/INN); PF-04449913;Glasdegib; GTPL8201; Glasdegib(PF-04449913); EX-A858; MolPort-035-789-706; SFNSLLSYNZWZQG-VQIMIIECSA-N; ZINC68251434; PF-913; BDBM50385635; 2640AH; AKOS027324121; CS-2
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Status
Approved
Structure
Formula
C21H22N6O
InChI
1S/C21H22N6O/c1-27-11-10-16(24-21(28)23-15-8-6-14(13-22)7-9-15)12-19(27)20-25-17-4-2-3-5-18(17)26-20/h2-9,16,19H,10-12H2,1H3,(H,25,26)(H2,23,24,28)/t16-,19-/m1/s1
InChIKey
SFNSLLSYNZWZQG-VQIMIIECSA-N
PubChem CID
25166913
TTD Drug ID
D0S5LO
INTEDE Drug ID
DR0774
Target Gene(s) and Their Upstream m6A Regulator, Together with the Effect of Target Gene(s) in Drug Response
The target genes involved in drug-target interaction (such as drug-metabolizing enzymes, drug transporters and therapeutic targets) and drug-mediated cell death signaling (including modulating DNA damage and repair capacity, escaping from drug-induced apoptosis, autophagy, cellular metabolic reprogramming, oncogenic bypass signaling, cell microenvironment, cell stemness, etc.) could be regulated by m6A regulator(s) and affected their corresponding drug response. You can browse detailed information on drug-related target gene(s) mediated by m6A regulators.
Cytochrome P450 2C8 (CYP2C8)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for Glasdegib. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of Glasdegib through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for Glasdegib. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of Glasdegib through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for Glasdegib. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Glasdegib through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
YTH domain-containing protein 2 (YTHDC2)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for Glasdegib. The YTH domain-containing protein 2 (YTHDC2) has potential in affecting the response of Glasdegib through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
Serine/threonine-protein kinase mTOR (mTOR)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for Glasdegib. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of Glasdegib through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [3], [4]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for Glasdegib. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of Glasdegib through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [4], [5]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for Glasdegib. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Glasdegib through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [4], [6]
YTH domain-containing family protein 1 (YTHDF1)
In total 1 mechanisms lead to this potential drug response
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for Glasdegib. The YTH domain-containing family protein 1 (YTHDF1) has potential in affecting the response of Glasdegib through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [4], [7]
YTH domain-containing family protein 2 (YTHDF2)
In total 1 mechanisms lead to this potential drug response
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for Glasdegib. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of Glasdegib through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [3], [4]
References
Ref 1 Methylation of adenosine at the N(6) position post-transcriptionally regulates hepatic P450s expression. Biochem Pharmacol. 2020 Jan;171:113697. doi: 10.1016/j.bcp.2019.113697. Epub 2019 Nov 7.
Ref 2 Metabolism, excretion and pharmacokinetics of [(14)C]glasdegib (PF-04449913) in healthy volunteers following oral administration. Xenobiotica. 2017 Dec;47(12):1064-1076. doi: 10.1080/00498254.2016.1261307. Epub 2017 Jan 3.
Ref 3 Targeting ATF4-dependent pro-survival autophagy to synergize glutaminolysis inhibition. Theranostics. 2021 Jul 25;11(17):8464-8479. doi: 10.7150/thno.60028. eCollection 2021.
Ref 4 Hedgehog inhibitors: a patent review (2013 - present). Expert Opin Ther Pat. 2015 May;25(5):549-65. doi: 10.1517/13543776.2015.1019864. Epub 2015 Mar 1.
Ref 5 The m6A methyltransferase METTL14 inhibits the proliferation, migration, and invasion of gastric cancer by regulating the PI3K/AKT/mTOR signaling pathway. J Clin Lab Anal. 2021 Mar;35(3):e23655. doi: 10.1002/jcla.23655. Epub 2020 Dec 12.
Ref 6 Methyltransferase-like 3 promotes the progression of lung cancer via activating PI3K/AKT/mTOR pathway. Clin Exp Pharmacol Physiol. 2022 Jul;49(7):748-758. doi: 10.1111/1440-1681.13647. Epub 2022 May 23.
Ref 7 YTHDF1 promotes hepatocellular carcinoma progression via activating PI3K/AKT/mTOR signaling pathway and inducing epithelial-mesenchymal transition. Exp Hematol Oncol. 2021 Jun 4;10(1):35. doi: 10.1186/s40164-021-00227-0.