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

General Information of Drug (ID: DM6I5GR)

• Drug Name: Promethazine Drug Info
• Synonyms: Antiallersin; Aprobit; Avomine; Camergan; Dimapp; Diphergan; Diprazin; Diprazine; Diprozin; Fargan; Fenazil; Fenetazina; Fenetazine; Genphen; Hiberna; Histargan; Iergigan; Isophenergan; Isopromethazine; Lercigan; Lergigan; Metaryl; Pelpica; Phargan; Phenargan; Phenerzine; Phensedyl; Pilothia; Pilpophen; Pipolphene; Proazaimine; Proazamine; Procit; Promacot; Promazinamide; Promergan; Promesan; Prometasin; Prometazin; Prometazina; Prometazine; Prometh; Promethacon; Promethaine; Promethazin; PromethazineHcl; Promethazinum; Promethegan; Promethiazine; Promezathine; Prorex; Protazine; Prothazin; Prothazine; Provigan; Pyrethia; Pyrethiazine; Remsed; Romergan; Rumergan; Tanidil; Thiergan; Valergine; Vallergine; Lilly 01516; Lilly 1516; RP 3277; SKF 1498; WY 509; A-91033; Atosil (TN); Avomine (TN); Fargan (TN); Farganesse (TN); Lergigan (TN); Phenergan (TN); Phenoject-50; Pro-50; Prometazina [INN-Spanish]; Promethazine [INN:BAN]; Promethazinum [INN-Latin]; Promethegan (TN); Prothiazine (TN); Receptozine (TN); Romergan (TN); Zipan-25; Dimethylamino-isopropyl-phenthiazin; Dimethylamino-isopropyl-phenthiazin [German]; Promethazine (JAN/INN)

Indication

Disease Entry	ICD 11	Status	REF
Hyperemesis gravidarum		Approved	[1]
Nausea	MD90	Approved	[2]
Seasonal allergic rhinitis	CA08.01	Approved	[1]
Urticaria	EB00-EB05	Approved	[1]
Vasomotor/allergic rhinitis	CA08	Approved	[1]
Vomiting	MD90	Approved	[1]
Middle East Respiratory Syndrome (MERS)	1D64	Investigative	[3]
Severe acute respiratory syndrome (SARS)	1D65	Investigative	[4]

• Therapeutic Class: Antiallergic Agents
• Cross-matching ID:
  PubChem CID: 4927
  ChEBI ID: CHEBI:8461
  CAS Number: CAS 60-87-7
  TTD Drug ID: DM6I5GR
  VARIDT Drug ID: DR00674
  INTEDE Drug ID: DR1353
  ACDINA Drug ID: D00561

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Histamine H1 receptor (H1R)	TTTIBOJ	HRH1_HUMAN	Antagonist	[5]
HUMAN clathrin-mediated endocytosis (RME)	TTAIY2U	.	Inhibitor	[4]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Approved	[6]
Cytochrome P450 2B6 (CYP2B6)	DEPKLMQ	CP2B6_HUMAN	Approved	[7]

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

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Histamine H1 receptor (H1R)	DTT	HRH1	5.972	5.7	5.816	6.002
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	3.307	5.005	3.921	5.327

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

• The Studied Disease: Hyperemesis gravidarum

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Histamine H1 receptor (H1R)	DTT	HRH1	6.74E-01	0.13	0.43
Cytochrome P450 2B6 (CYP2B6)	DME	CYP2B6	4.32E-01	4.39E-02	4.30E-01
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	8.70E-01	2.98E-02	1.22E-01

References

• [1] Promethazine 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: 7282).
• [3] Repurposing of clinically developed drugs for treatment of Middle East respiratory syndrome coronavirus infection. Antimicrob Agents Chemother. 2014 Aug;58(8):4885-93.
• [4] Therapeutic options for the 2019 novel coronavirus (2019-nCoV). Nat Rev Drug Discov. 2020 Mar;19(3):149-150.
• [5] Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79.
• [6] Akathisia with combined use of midodrine and promethazine. JAMA. 2006 May 3;295(17):2000-1. Letter
• [7] Bupropion and 4-OH-bupropion pharmacokinetics in relation to genetic polymorphisms in CYP2B6. Pharmacogenetics. 2003 Oct;13(10):619-26.