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

General Information of Drug (ID: DMJZHT1)

Drug Name

Tadalafil Drug Info

Synonyms

ADCIRCA; Acdirca; Cialis; Tadanafil; Lilly brand of tadalafil; Tadalafil [USAN]; GF 196960; IC 351; ICOS 351; Ic351; Cialis (TN); GF-196960; IC-351; KS-1117; Tadalafil (JAN/USAN/INN); Cialis, GF 196960, IC 351, ICOS 351, Tadalafil; (6R,12aR)-2,3,6,7,12,12a-Hexahydro-2-methyl-6-(3,4-(methylenedioxy)phenyl) pyrazino(1',2':1,6)pyrido(3,4-b)indole-1,4-dione; (6R,12aR)-2,3,6,7,12,12a-Hexahydro-2-methyl-6-(3,4-methylenedioxyphenyl)pyrazino(1',2':1,6)pyrido(3,4-b)indole-1,4-dione; (6R-trans)-6-(1,3-Benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl-pyrazino(1',2':1,6)pyrido(3,4-b)indole-1,4-dione

Indication

Disease Entry	ICD 11	Status	REF
Benign prostatic hyperplasia	GA90	Approved	[1]
Erectile dysfunction	HA01.1	Approved	[2]
Plasma cell myeloma	2A83.1	Approved	[1]
Pulmonary hypertension	BB01	Approved	[1]
Priapism		Investigative	[1]

Therapeutic Class

Antiimpotence Agents

Cross-matching ID

PubChem CID: 110635
ChEBI ID: CHEBI:71940
CAS Number: CAS 171596-29-5
TTD Drug ID: DMJZHT1
VARIDT Drug ID: DR01260
INTEDE Drug ID: DR1525
ACDINA Drug ID: D00649

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Phosphodiesterase 5A (PDE5A)	TTJ0IQB	PDE5A_HUMAN	Inhibitor	[3]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[4]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Approved	[5]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Approved	[5]

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

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Phosphodiesterase 5A (PDE5A)	DTT	PDE5A	3.632	3	3.632	4.271
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	10.08	7.207	5.403	9.211
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

Benign prostatic hyperplasia

ICD Disease Classification

GA90

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Phosphodiesterase 5A (PDE5A)	DTT	PDE5A	1.60E-01	-0.25	-0.99
P-glycoprotein 1 (ABCB1)	DTP	P-GP	2.16E-04	-1.07E+00	-2.77E+00
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	3.78E-02	4.07E-01	1.09E+00
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	3.90E-02	-3.45E-01	-1.49E+00

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Tadalafil FDA Label
2	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: 7299).
3	Pulmonary arterial hypertension: the most devastating vascular complication of systemic sclerosis. Rheumatology (Oxford). 2009 Jun;48 Suppl 3:iii25-31.
4	In Vitro P-Glycoprotein-Mediated Transport of Tadalafil: A Comparison with Sildenafil. Biol Pharm Bull. 2017;40(8):1314-1319.
5	Contribution of CYP3A isoforms to dealkylation of PDE5 inhibitors: a comparison between sildenafil N-demethylation and tadalafil demethylenation. Biol Pharm Bull. 2015;38(1):58-65.