Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTM5Q4V)

• DTT Name: Organic cation transporter 1
• Synonyms: Solute carrier family 22 member 1; hOCT1; SLC22A1
• Gene Name: SLC22A1
• BioChemical Class: Single Protein
• UniProt ID: S22A1_HUMAN
• TTD ID: TE0106
• Sequence:
  MPTVDDILEQVGESGWFQKQAFLILCLLSAAFAPICVGIVFLGFTPDHHCQSPGVAELSQ
  RCGWSPAEELNYTVPGLGPAGEAFLGQCRRYEVDWNQSALSCVDPLASLATNRSHLPLGP
  CQDGWVYDTPGSSIVTEFNLVCADSWKLDLFQSCLNAGFLFGSLGVGYFADRFGRKLCLL
  GTVLVNAVSGVLMAFSPNYMSMLLFRLLQGLVSKGNWMAGYTLITEFVGSGSRRTVAIMY
  QMAFTVGLVALTGLAYALPHWRWLQLAVSLPTFLFLLYYWCVPESPRWLLSQKRNTEAIK
  IMDHIAQKNGKLPPADLKMLSLEEDVTEKLSPSFADLFRTPRLRKRTFILMYLWFTDSVL
  YQGLILHMGATSGNLYLDFLYSALVEIPGAFIALITIDRVGRIYPMAMSNLLAGAACLVM
  IFISPDLHWLNIIIMCVGRMGITIAIQMICLVNAELYPTFVRNLGVMVCSSLCDIGGIIT
  PFIVFRLREVWQALPLILFAVLGLLAAGVTLLLPETKGVALPETMKDAENLGRKAKPKEN
  TIYLKVQTSEPSGT
• Function: Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine, and metformin.

The Drug Transporter (DTP) Role of This DTT

• DTT DTP Name: Organic cation transporter 1 (SLC22A1) DTP Info
• Gene Name: SLC22A1

65 Approved Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Acebutolol	DM0TI4U	Hypertension	BA00-BA04	Approved	[1]
Acetylcholine	DMDF79Z	Cataract	9B10	Approved	[2]
Aciclovir	DMYLOVR	Genital herpes	1A94	Approved	[3]
Amiloride	DMRTSGP	Congestive heart failure	BD10	Approved	[4]
Atenolol	DMNKG1Z	Angina pectoris	BA40	Approved	[4]
Atropine	DMEN6X7	Organophosphate poisoning	NE6Z	Approved	[4]
Auranofin	DMWE2N4	Inflammatory arthritis	FA2Z	Approved	[5]
Buformin	DMX82DO	N. A.	N. A.	Approved	[6]
Cimetidine	DMH61ZB	Acid-reflux disorder	DA22	Approved	[4]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[7]
Citalopram	DM2G9AE	Acute coronary syndrome	BA41	Approved	[8]
Cladribine	DM3JDRP	Hairy cell leukaemia	2A82.2	Approved	[6]
Clidinium	DMUMQZ0	Abdominal stomach pain	DD91.4	Approved	[4]
Clonidine	DM6RZ9Q	Attention deficit hyperactivity disorder	6A05.Z	Approved	[9]
Codeine	DMJX6ZG	Allergic rhinitis	CA08.0	Approved	[10]
Cytarabine	DMZD5QR	Acute lymphoblastic leukaemia	2A85	Approved	[6]
Debrisoquin	DMC50ME	Hypertension	BA00-BA04	Approved	[11]
Desipramine	DMT2FDC	Attention deficit hyperactivity disorder	6A05.Z	Approved	[1]
Dinoprostone	DMTYOPD	Medical abortion	JA00.1Z	Approved	[12]
Disopyramide	DM5SYZP	Long QT syndrome	BC65.0	Approved	[4]
Dopamine	DMPGUCF	Acromegaly	5A60.0	Approved	[8]
Epinephrine	DM3KJBC	Acute asthma	CA23	Approved	[6]
Fenoterol	DMIP3ZV	Asthma	CA23	Approved	[4]
Fexofenadine	DM17ONX	Allergic rhinitis	CA08.0	Approved	[13]
Formoterol	DMSOURV	Allergic asthma	CA23.0	Approved	[4]
Ganciclovir	DM1MBYQ	Cytomegalovirus infection	1D82	Approved	[3]
Glycopyrrolate	DM2M3ZA	Anaesthesia	9A78.6	Approved	[4]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[14]
Indacaterol	DMQJHR7	Chronic obstructive pulmonary disease	CA22	Approved	[4]
Ipratropium	DMFQ320	Obstructive lung disease	CA22.Z	Approved	[4]
Lamivudine	DMI347A	Chronic HBV infection	1E51.0Z	Approved	[15]
Lamotrigine	DM8SXYG	Bipolar disorder	6A60	Approved	[16]
Metformin	DM89QE1	Colorectal carcinoma		Approved	[17]
Metoclopramide	DMFA5MY	Nausea	MD90	Approved	[4]
Naratriptan	DMO50U2	Headache	8A80-8A84	Approved	[18]
Nizatidine	DMGFV3Z	Acid-reflux disorder	DA22	Approved	[4]
Norepinephrine	DMOUC09	Alopecia	ED70	Approved	[8]
Oxaliplatin	DMQNWRD	Adenocarcinoma	2D40	Approved	[19]
Oxyphenonium	DMMQHOZ	Visceral spasms	MD81.4	Approved	[4]
Pentamidine	DMHZJCG	African trypanosomiasis	1F51	Approved	[20]
Perphenazine	DMA4MRX	Schizophrenia	6A20	Approved	[4]
Phenoxybenzamine	DM8KSQH	Malignant essential hypertension	BA00	Approved	[1]
Pramipexole	DMNMW9R	Parkinson disease	8A00.0	Approved	[21]
Prazosin	DMCD9YG	Benign prostatic hyperplasia	GA90	Approved	[1]
Procainamide	DMNMXR8	Ventricular arrhythmias	BC71	Approved	[4]
Procaterol	DM1M0Q4	Asthma	CA23	Approved	[4]
Propranolol	DM79NTF	Angina pectoris	BA40	Approved	[9]
Quinine	DMSWYF5	Malaria	1F40-1F45	Approved	[22]
Ranitidine	DM0GUSX	Gastric ulcer	DA60	Approved	[23]
Rizatriptan	DMDJMA3	Migraine	8A80	Approved	[18]
Salbutamol	DMN9CWF	Acute asthma	CA23	Approved	[4]
Sitagliptin	DMGDKXN	Cystic fibrosis	CA25	Approved	[24]
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[25]
Sumatriptan	DMVYXR8	Cluster headache	8A81.0	Approved	[4]
Terbutaline	DMD4381	Asthma	CA23	Approved	[4]
Tiotropium	DMFDC0Q	Chronic obstructive pulmonary disease	CA22	Approved	[4]
Triamterene	DM2HU9I	Congestive heart failure	BD10	Approved	[4]
Trimethoprim	DMM7CHK	Acute otitis media	AB00	Approved	[4]
Trospium chloride	DM32XZT	Discovery agent	N.A.	Approved	[26]
Tubocurarine	DMBZIVP	Anaesthesia	9A78.6	Approved	[6]
Varenicline	DMMUOLJ	Drug dependence		Approved	[4]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[1]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[6]
Zolmitriptan	DM1IB4Q	Migraine	8A80	Approved	[18]
Berberine	DMC5Q8X	N. A.	N. A.	Phase 4	[27]

5 Clinical Trial Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Spermidine	DMVJNFI	Plaque psoriasis	EA90.0	Phase 3	[6]
N1-methylnicotinamide	DM16PWF	Hyperlipidemia	5C80.Z	Phase 2/3	[28]
Camostat	DMQ7UL8	Cystic fibrosis	CA25	Phase 2	[4]
YM155	DM5Q1W4	Breast cancer	2C60-2C65	Phase 2	[29]
PGF2alpha	DM4XAU7	Solid tumour/cancer	2A00-2F9Z	Clinical trial	[30]

1 Discontinued Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Phenformin	DMQ52JG	Diabetic complication	5A2Y	Withdrawn from market	[4]

3 Preclinical Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(R)-Xamoterol	DMXWD08	N. A.	N. A.	Preclinical	[4]
(S)-Xamoterol	DM1ZQ5G	N. A.	N. A.	Preclinical	[4]
N-methylpyridinium	DMVUKEW	N. A.	N. A.	Preclinical	[31]

6 Investigative Drug(s) Transported by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
benzamil	DM57SVW	Discovery agent	N.A.	Investigative	[4]
CHOLINE	DM5D9YK	Insomnia	7A00-7A0Z	Investigative	[6]
PHENCYCLIDINE	DMQBEYX	Discovery agent	N.A.	Investigative	[32]
Tetramethylammonium Ion	DMLEPYN	Discovery agent	N.A.	Investigative	[33]
tyramine	DM4UXT1	Discovery agent	N.A.	Investigative	[6]
[14C]TEA	DM6SFYH	Discovery agent	N.A.	Investigative	[34]

References

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• [3] Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. J Pharmacol Exp Ther. 2002 Mar;300(3):918-24.
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• [26] Expression of drug transporters and drug metabolizing enzymes in the bladder urothelium in man and affinity of the bladder spasmolytic trospium chloride to transporters likely involved in its pharmacokinetics. Mol Pharm. 2015 Jan 5;12(1):171-8.
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• [34] Involvement of human organic cation transporter 1 in the hepatic uptake of 1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazolium bromide (YM155 monobromide), a novel, small molecule survivin suppressant. Drug Metab Dispos. 2009 Sep;37(9):1856-63.