SERTINDOLE

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C24H26ClFN4O
Molecular Weight	440.941
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

FC1=CC=C(C=C1)N2C=C(C3CCN(CCN4CCNC4=O)CC3)C5=C2C=CC(Cl)=C5

InChI

InChIKey=GZKLJWGUPQBVJQ-UHFFFAOYSA-N

InChI=1S/C24H26ClFN4O/c25-18-1-6-23-21(15-18)22(16-30(23)20-4-2-19(26)3-5-20)17-7-10-28(11-8-17)13-14-29-12-9-27-24(29)31/h1-6,15-17H,7-14H2,(H,27,31)

HIDE SMILES / InChI

Molecular Formula	C24H26ClFN4O
Molecular Weight	440.941
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.drugbank.ca/drugs/DB06144
Curator's Comment: description was created based on several sources, including https://www.drugs.com/international/sertindole.html | https://www.ncbi.nlm.nih.gov/pubmed/23218776 | https://www.ncbi.nlm.nih.gov/pubmed/12747773 | https://www.ncbi.nlm.nih.gov/pubmed/20857909 | https://www.ncbi.nlm.nih.gov/pubmed/22791154 | https://www.ncbi.nlm.nih.gov/pubmed/22850268

Sertindole (brand names: "Serdolect" and "Serlect") is an antipsychotic medication. Sertindole was developed by the Danish pharmaceutical company Lundbeck and marketed under license by Abbott Labs. Like other atypical antipsychotics, it has activity at dopamine and serotonin receptors in the brain. It is used in the treatment of schizophrenia. Sertindole is not approved for use in the United States and was discontinued in Australia in January 2014. In Europe, sertindole was approved and marketed in 19 countries from 1996, but its marketing authorization was suspended by the European Medicines Agency in 1998 and the drug was withdrawn from the market. In 2002, based on new data, the EMA's CHMP suggested that Sertindole could be reintroduced for restricted use in clinical trials, with strong safeguards including extensive contraindications and warnings for patients at risk of cardiac dysrhythmias, a recommended reduction in maximum dose from 24 mg to 20 mg in all but exceptional cases, and extensive ECG monitoring requirement before and during treatment.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Dopamine D2 receptor 311 Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23218776	Antagonist 2849	0.45 nM [Ki]
Serotonin 2a (5-HT2a) receptor 237 Target ID: CHEMBL224 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12747773	Antagonist 2849	0.6 nM [Ki]
Serotonin 2c (5-HT2c) receptor 131 Target ID: CHEMBL225 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20857909	Antagonist 2849	0.2 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Schizophrenia 305 Sources: https://clinicaltrials.gov/ct2/show/NCT00763438	Primary		Approved 8583	Sertindole Approved Use Unknown

C_max

Value	Dose	Analyte	Population
1.41 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.78 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.41 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.34 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
0.89 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
1.83 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
0.97 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
53.13 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
38.34 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
43.91 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
34.06 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
63.74 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
43.29 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
57.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
51.58 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
3.2 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.2 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.4 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
1.7 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
3.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
1.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
3.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
1.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
24.2 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
24.3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
14 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
41.5 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
13.7 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
31.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
14.7 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
953.2 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
723.8 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
839.4 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
645.4 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1231.4 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
846.5 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
1084.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
925.4 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
346 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
494 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
225 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
320 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
323 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
442 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
282 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
349 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
84.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
99.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
90.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
108.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
99 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
97.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
101.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
110.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	12 mg 1 times / day multiple, oral dose: 12 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
86 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
242 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
75 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
150 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
93 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
135 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
73 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
165 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDROSERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED

F_unbound

Value	Dose	Analyte	Population
0.5% OTHER GOV'T https://www.ema.europa.eu/en/documents/referral/opinion-following-article-36-referral-sertindole-international-non-proprietary-name-inn-sertindole_en.pdf#page=31		SERTINDOLE plasma	Homo sapiens
0.64% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.57% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.55% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
0.56% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9284851/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	SERTINDOLE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
0.55% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/		SERTINDOLE plasma	Homo sapiens population: UNKNOWN age: ADULT sex: MALE food status: UNKNOWN
0.82% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9218930/		SERTINDOLE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
24 mg 1 times / day multiple, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: multiple Dose: 24 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/22609816/	unhealthy, ADOLESCENT Health Status: unhealthy Age Group: ADOLESCENT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/22609816/	Disc. AE: Ejaculation failure... Other AEs: Suicidal ideation... AEs leading to discontinuation/dose reduction: Ejaculation failure (4%) Other AEs: Suicidal ideation (2%) Sources: https://pubmed.ncbi.nlm.nih.gov/22609816/
1792 mg single, oral Overdose\|Highest recorded dose Dose: 1792 mg Route: oral Route: single Dose: 1792 mg Sources: https://pubmed.ncbi.nlm.nih.gov/20163279/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20163279/	Disc. AE: Somnolence... AEs leading to discontinuation/dose reduction: Somnolence Sources: https://pubmed.ncbi.nlm.nih.gov/20163279/
17 mg 1 times / day multiple, oral Recommended Dose: 17 mg, 1 times / day Route: oral Route: multiple Dose: 17 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/22850268/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/22850268/	Disc. AE: QT prolonged... AEs leading to discontinuation/dose reduction: QT prolonged Sources: https://pubmed.ncbi.nlm.nih.gov/22850268/

AEs

AE	Significance	Dose	Population
Suicidal ideation	2%	24 mg 1 times / day multiple, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: multiple Dose: 24 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/22609816/	unhealthy, ADOLESCENT Health Status: unhealthy Age Group: ADOLESCENT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/22609816/
Ejaculation failure	4% Disc. AE	24 mg 1 times / day multiple, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: multiple Dose: 24 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/22609816/	unhealthy, ADOLESCENT Health Status: unhealthy Age Group: ADOLESCENT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/22609816/
Somnolence	Disc. AE	1792 mg single, oral Overdose\|Highest recorded dose Dose: 1792 mg Route: oral Route: single Dose: 1792 mg Sources: https://pubmed.ncbi.nlm.nih.gov/20163279/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20163279/
QT prolonged	Disc. AE	17 mg 1 times / day multiple, oral Recommended Dose: 17 mg, 1 times / day Route: oral Route: multiple Dose: 17 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/22850268/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/22850268/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252 substrate 1946	inhibitor 2438	inhibitor 2507 substrate 1388	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
MRP4 290 MRP2 499 P-gp 1741 MRP3 246 BSEP 550 CYP19A1 429 CYP2C19 2057 CYP1A2 2153	P-gp 2052

Drug as perpetrator

Target	Modality	Activity
CYP19A1 430	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/60149#section=BioAssay-Results Page: 52.0	inconclusive [IC50 23.7101 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/60149#section=BioAssay-Results Page: 71.0	inconclusive [IC50 38.9018 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/60149#section=BioAssay-Results Page: 70.0	inconclusive [IC50 38.9018 uM]
MRP2 625	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1NzQ4IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyNzEzIn19	no [IC50 >133 uM]
MRP3 326	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1OTE4IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyNzEzIn19	no [IC50 >133 uM]
MRP4 345	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwxNzQzMTI4IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyNzEzIn19	no [IC50 >133 uM]
CYP1A2 2333	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/60149#section=BioAssay-Results Page: 147.0	no
CYP2C19 2141	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/60149#section=BioAssay-Results Page: 147.0	no
BSEP 554	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw2MDIwIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyNzEzIn19	weak [IC50 82.7 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/60149#section=BioAssay-Results Page: 18.0	yes [IC50 1.5487 uM]
P-gp 1932	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw0MzAyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyNzEzIn19	yes [IC50 6.5 uM]

Drug as victim

Target	Modality	Activity	Clinical evidence
P-gp 2052	substrate 4014 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/60149#section=BioAssay-Results Page: 45 \| 125	inconclusive
CYP2D6 1388	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/10688273/ \| https://pubmed.ncbi.nlm.nih.gov/20856845/	yes
CYP3A4 1946	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/10688273/ \| https://pubmed.ncbi.nlm.nih.gov/20856845/ \| https://pubmed.ncbi.nlm.nih.gov/9505999/	yes	weak (co-administration study) Comment: Erythromycin increased Sertindole Cmax by 1.15-fold Sources: https://pubmed.ncbi.nlm.nih.gov/10688273/ \| https://pubmed.ncbi.nlm.nih.gov/20856845/ \| https://pubmed.ncbi.nlm.nih.gov/9505999/

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMTI3MTMifX0=

PubMed

Title	Date	PubMed
Metabolic drug interactions with newer antipsychotics: a comparative review.	2007-01	17214606
Comparing sertindole to other new generation antipsychotics on preferential dopamine output in limbic versus striatal projection regions: mechanism of action.	2006-12-01	16952163
Pharmacological treatment of primary negative symptoms in schizophrenia: a systematic review.	2006-12	16930948
Beat-to-Beat variability of repolarization determines proarrhythmic outcome in dogs susceptible to drug-induced torsades de pointes.	2006-09-19	16979017
Sertindole: efficacy and safety in schizophrenia.	2006-09	16925508
Chlorpromazine, clozapine and olanzapine inhibit anionic amino acid transport in cultured human fibroblasts.	2006-09	16699818
Classical as well as novel antipsychotic drugs increase self-stimulation threshold in the rat--similar mechanism of action?	2006-08-21	16860313
Sertindole, in contrast to clozapine and olanzapine, does not disrupt water maze performance after acute or chronic treatment.	2006-08-07	16806167
Haloperidol dose when used as active comparator in randomized controlled trials with atypical antipsychotics in schizophrenia: comparison with officially recommended doses.	2006-06	16848649
Effects of antipsychotic drugs on I(to), I (Na), I (sus), I (K1), and hERG: QT prolongation, structure activity relationship, and network analysis.	2006-06	16715368
Pharmacological treatment of ambulatory schizophrenic patients in Belgium.	2006-05-30	16734909
New insights about HERG blockade obtained from protein modeling, potential energy mapping, and docking studies.	2006-05-01	16413785
Myocardium distribution of sertindole and its metabolite dehydrosertindole in guinea-pigs.	2006-05	16419145
Comparative evaluation of HERG currents and QT intervals following challenge with suspected torsadogenic and nontorsadogenic drugs.	2006-03	16278312
The effectiveness of atypical antipsychotics for the treatment of aggression and psychosis in Alzheimer's disease.	2006-01-25	16437455
A double-blind, controlled study of sertindole versus risperidone in the treatment of moderate-to-severe schizophrenia.	2006-01	16317317
A dopaminergic deficit hypothesis of schizophrenia: the path to discovery.	2006	16640125
The German Research Network on Schizophrenia--impact on the management of schizophrenia.	2006	16640122
Sertindole : a review of its use in schizophrenia.	2006	16529528
Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist.	2005-12	16135699
QTc interval prolongation and antipsychotic drug treatments: focus on sertindole.	2005-12	15963244
Treatment with the new antipsychotic sertindole for late-occurring undesirable movement effects.	2005-11	16192844
Generalization to atypical antipsychotic drugs depends on training dose in rats trained to discriminate 1.25 mg/kg clozapine versus 5.0 mg/kg clozapine versus vehicle in a three-choice drug discrimination task.	2005-11	16170228
Interactions between neuroleptics and CYP2C6 in rat liver--in vitro and ex vivo study.	2005-09-14	16382211
Direct effects of neuroleptics on the activity of CYP2A in the liver of rats.	2005-09-14	16382210
Atypical antipsychotics produce within-session decrements on self-stimulation of the rat medial prefrontal cortex.	2005-09-01	15970521
Comparison of methanol and acetonitrile as solvents for the separation of sertindole and its major metabolites by capillary zone electrophoresis.	2005-09	16097029
Neuropsychological measures of attention and memory function in schizophrenia: relationships with symptom dimensions and serum monoamine activity.	2005-08-09	16091141
Hostility and violence of acute psychiatric inpatients.	2005-07-29	16053528
Sertindole for schizophrenia.	2005-07-20	16034864
Current therapy issues and unmet clinical needs in the treatment of schizophrenia: a review of the new generation antipsychotics.	2005-07	15933479
Exploring blocker binding to a homology model of the open hERG K+ channel using docking and molecular dynamics methods.	2005-05-23	15893317
Unbiased descriptor and parameter selection confirms the potential of proteochemometric modelling.	2005-03-10	15760465
Antipsychotics lack alpha 1A/B adrenoceptor subtype selectivity in the rat.	2005-03	15695070
Choice of cardiac tissue plays an important role in the evaluation of drug-induced prolongation of the QT interval in vitro in rabbit.	2005-02-22	15978848
Simplified ultraviolet liquid chromatographic method for determination of sertindole, dehydrosertindole and norsertindole, in human plasma.	2005-01-05	15607708
Inhibition of rat liver CYP2D in vitro and after 1-day and long-term exposure to neuroleptics in vivo-possible involvement of different mechanisms.	2005-01	15572279
Atypical antipsychotics: from potassium channels to torsade de pointes and sudden death.	2005	15649104
Possible induction of mania or hypomania by atypical antipsychotics: an updated review of reported cases.	2004-11	15554769
[Psychotropics and weight gain].	2004-08-25	15468580
Determination of myocardium to plasma concentration ratios of five antipsychotic drugs: comparison with their ability to induce arrhythmia and sudden death in clinical practice.	2004-08-15	15289090
Evidence-based pharmacotherapy of schizophrenia.	2004-06	15043765
Atypical antipsychotics: pharmacokinetics, therapeutic drug monitoring and pharmacological interactions.	2004-02	14965232
[Current pharmacotherapy of schizophrenia].	2004-01-18	15027331
Impact of atypical antipsychotics on quality of life in patients with schizophrenia.	2004	15521791
Case histories illustrating the utility of sertindole in clinical practice.	2004	15461314
A review of the efficacy, tolerability and safety of sertindole in clinical trials.	2004	15461313
Introduction to sertindole in clinical practice.	2004	15461311
Cardiovascular side effects of new antidepressants and antipsychotics: new drugs, old concerns?	2004	15320756
Sertindole (Serdolect): preclinical and clinical findings of a new atypical antipsychotic.	1997-11	15989577

Patents

Sample Use Guides

In Vivo Use Guide

The sertindole treatment period consisted of a 16-day up-titration period (initiated at 4 mg/day and the dose was increased by 4 mg every fourth day to reach the effective target dose of 16 mg/day at the 16th day), followed by a flexible-dose maintenance period (12, 16, or 20 mg/day according to the investigator’s judgment).

Route of Administration: Oral

In Vitro Use Guide

SH-SY5Y cells stably expressing GFP-LC3 (SY5Y/GFP-LC3) were treated with Sertindole (10 μM) for 24 h. The cells were then fixed and observed by fluorescence microscopy or electron microscopy.

Substance Class	Chemical Created by `admin` on `Wed Apr 02 07:43:03 GMT 2025` Edited by `admin` on `Wed Apr 02 07:43:03 GMT 2025`
Record UNII	GVV4Z879SP
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

SERTINDOLE

Official Name

English

SERDOLECT

Preferred Name

English

LU-23-174

Code

English

SERTINDOLE [USAN]

Common Name

English

Sertindole [WHO-DD]

Common Name

English

sertindole [INN]

Common Name

English

SERTINDOLE [VANDF]

Common Name

English

2-IMIDAZOLIDINONE, 1-(2-(4-(5-CHLORO-1-(4-FLUOROPHENYL)-1H-INDOL-3-YL)-1-PIPERIDINYL)ETHYL)-

Systematic Name

English

SERTINDOLE [MI]

Common Name

English

ZERDOL

Brand Name

English

SERLECT

Brand Name

English

LU 23-174

Code

English

SERTINDOLE [MART.]

Common Name

English

Classification Tree Code System Code

WHO-VATC

QN05AE03