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

General Information of Drug (ID: DMF98Q0)

Drug Name

Momelotinib Drug Info

Synonyms

Cyt387; 1056634-68-4; MOMELOTINIB; Cyt-387; N-(Cyanomethyl)-4-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)benzamide; CYT 387; CYT 11387; UNII-6O01GMS00P; N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide; 6O01GMS00P; CHEMBL1078178; AK102858; N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide; N-(cyanomethyl)-4-(2-{[4-(morpholin-4-yl)phenyl]amino}pyrimidin-4-yl)benzamide; CYT387 sulfate salt; N-(Cyanomethyl)-4-(2-((4-morpholinophenyl)-amino)pyrimidin-4-yl)benzamide

Indication

Disease Entry	ICD 11	Status	REF
Myelofibrosis	2A20.2	Approved	[1]
Polycythemia vera	2A20.4	Phase 2	[2]
Thrombocythemia	3B63	Phase 2	[2]

Cross-matching ID

PubChem CID: 25062766
ChEBI ID: CHEBI:91407
CAS Number: CAS 1056634-68-4
TTD Drug ID: DMF98Q0
INTEDE Drug ID: DR1880

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Janus kinase 1 (JAK-1)	TT6DM01	JAK1_HUMAN	Modulator	[1]
Janus kinase 2 (JAK-2)	TTRMX3V	JAK2_HUMAN	Modulator	[3]

------------------------------------------------------------------------------------

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Phase 3	[4]
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Phase 3	[4]
Mephenytoin 4-hydroxylase (CYP2C19)	DEGTFWK	CP2CJ_HUMAN	Phase 3	[4]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_HUMAN	Phase 3	[4]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_HUMAN	Phase 3	[4]

------------------------------------------------------------------------------------

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Janus kinase 2 (JAK-2)	DTT	JAK2	4.957	5.257	4.986	4.784
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	9.791	3.744	3.413	1.609
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	10.036	5.779	6.508	6.481
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	7.867	5.142	5.52	7.08
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	11.76	5.931	6.164	9.423
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	11.692	6.58	4.984	9.089

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease

Myelofibrosis

ICD Disease Classification

2A20.2

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Janus kinase 2 (JAK-2)	DTT	JAK2	2.46E-01	-0.41	-0.6
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	6.03E-01	7.61E-02	6.10E-01
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	1.93E-01	3.11E-01	8.10E-01
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	1.67E-02	8.33E-01	1.75E+00
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	1.21E-01	5.16E-01	1.33E+00
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	1.23E-01	4.92E-01	1.13E+00

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	FDA Approved Drug Products from FDA Official Website. 2023. Application Number: 216873
2	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3	Genetic determinants of response and survival in momelotinib-treated patients with myelofibrosis.Leukemia.2015 Mar;29(3):741-4.
4	Pharmacokinetics and disposition of momelotinib revealed a disproportionate human metabolite-resolution for clinical development. Drug Metab Dispos. 2018 Mar;46(3):237-247.