U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C21H33N3O.2ClH
Molecular Weight 416.428
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SITAMAQUINE DIHYDROCHLORIDE

SMILES

Cl.Cl.CCN(CC)CCCCCCNC1=CC(OC)=CC2=C1N=CC=C2C

InChI

InChIKey=AFMFKGVIHLNIEO-UHFFFAOYSA-N
InChI=1S/C21H33N3O.2ClH/c1-5-24(6-2)14-10-8-7-9-12-22-20-16-18(25-4)15-19-17(3)11-13-23-21(19)20;;/h11,13,15-16,22H,5-10,12,14H2,1-4H3;2*1H

HIDE SMILES / InChI
Molecular Formula C21H33N3O
Molecular Weight 343.5062
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/16945323

Sitamaquine (WR-6026) is an orally active 8-aminoquinoline analog in development by the Walter Reed Army Institute, in collaboration with GlaxoSmithKline (formerly SmithKline Beecham), for the potential treatment of visceral leishmaniasis. Phase III trials for the treatment of visceral leishmaniasis had been initiated by March 2002, at which time GlaxoSmithKline hoped to file an MAA in 2003. By 1999, the compound had also undergone phase I trials in HIV-infected individuals for the treatment of Pneumocystis carinii infection. Preclinical studies have been conducted in primates and rodents for the potential treatment of Babesia microti infection.

Originator

Approval Year

Unknown
139594
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
 29.2 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
Phase II
1132
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
484.3 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/10235511
150 mg 1 times / day multiple, oral
dose: 150 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SITAMAQUINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
577 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21633025
2 mg/kg single, oral
dose: 2 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
SITAMAQUINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
451 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21633025
2 mg/kg 1 times / day multiple, oral
dose: 2 mg/kg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SITAMAQUINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
503 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21633025
2 mg/kg 1 times / day multiple, oral
dose: 2 mg/kg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SITAMAQUINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
639 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21633025
2 mg/kg 1 times / day single, oral
dose: 2 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
SITAMAQUINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
6916 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/10235511
150 mg 1 times / day multiple, oral
dose: 150 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SITAMAQUINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
7147 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21633025
2 mg/kg single, oral
dose: 2 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
SITAMAQUINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
7723 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21633025
2 mg/kg 1 times / day multiple, oral
dose: 2 mg/kg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SITAMAQUINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
8350 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21633025
2 mg/kg 1 times / day multiple, oral
dose: 2 mg/kg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SITAMAQUINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
8574 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21633025
2 mg/kg 1 times / day single, oral
dose: 2 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
SITAMAQUINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
19.3 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21633025
2 mg/kg 1 times / day multiple, oral
dose: 2 mg/kg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SITAMAQUINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
18.3 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21633025
2 mg/kg 1 times / day multiple, oral
dose: 2 mg/kg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SITAMAQUINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
120 mg 1 times / day multiple, oral
MTD
Dose: 120 mg, 1 times / day
Route: oral
Route: multiple
Dose: 120 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 18
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 18
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
DLT: Elevated triglycerides...
Disc. AE: Skin rash, Nausea...
Dose limiting toxicities:
Elevated triglycerides (5.6%)
AEs leading to
discontinuation/dose reduction:
Skin rash (11.1%)
Nausea (5.6%)
Vomiting (5.6%)
Headache (5.6%)
CPK increased (5.6%)
LDH increased (5.6%)
AST increased (5.6%)
ALT increased (5.6%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
150 mg 1 times / day multiple, oral
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 8
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
DLT: Methemoglobinemia, Methemoglobinemia...
Disc. AE: Histoplasmosis, Fever...
Dose limiting toxicities:
Methemoglobinemia (12.5%)
Methemoglobinemia (37.5%)
Elevated triglycerides (12.5%)
AEs leading to
discontinuation/dose reduction:
Histoplasmosis (12.5%)
Fever (12.5%)
Flushing (12.5%)
Skin rash (12.5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
2.5 mg/kg 1 times / day multiple, oral
Studied dose
Dose: 2.5 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16354802
Page: p.1008
unhealthy, CHILD,ADULT
n = 28
Health Status: unhealthy
Condition: visceral leishmaniasis
Age Group: CHILD,ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 28
Sources:
https://pubmed.ncbi.nlm.nih.gov/16354802
Page: p.1008
Disc. AE: Bone marrow depression, Acute renal failure...
AEs leading to
discontinuation/dose reduction:
Bone marrow depression (3.6%)
Acute renal failure (3.6%)
Bone marrow depression (3.6%)
Cardio-respiratory failure (grade 5, 3.6%)
Nephrotic syndrome (7.2%)
Glomerulonephritis (7.2%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/16354802
Page: p.1008
AEs

AEs

AESignificanceDosePopulation
Skin rash 11.1%
Disc. AE
120 mg 1 times / day multiple, oral
MTD
Dose: 120 mg, 1 times / day
Route: oral
Route: multiple
Dose: 120 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 18
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 18
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
Elevated triglycerides 5.6%
DLT
120 mg 1 times / day multiple, oral
MTD
Dose: 120 mg, 1 times / day
Route: oral
Route: multiple
Dose: 120 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 18
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 18
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
ALT increased 5.6%
Disc. AE
120 mg 1 times / day multiple, oral
MTD
Dose: 120 mg, 1 times / day
Route: oral
Route: multiple
Dose: 120 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 18
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 18
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
AST increased 5.6%
Disc. AE
120 mg 1 times / day multiple, oral
MTD
Dose: 120 mg, 1 times / day
Route: oral
Route: multiple
Dose: 120 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 18
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 18
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
CPK increased 5.6%
Disc. AE
120 mg 1 times / day multiple, oral
MTD
Dose: 120 mg, 1 times / day
Route: oral
Route: multiple
Dose: 120 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 18
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 18
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
Headache 5.6%
Disc. AE
120 mg 1 times / day multiple, oral
MTD
Dose: 120 mg, 1 times / day
Route: oral
Route: multiple
Dose: 120 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 18
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 18
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
LDH increased 5.6%
Disc. AE
120 mg 1 times / day multiple, oral
MTD
Dose: 120 mg, 1 times / day
Route: oral
Route: multiple
Dose: 120 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 18
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 18
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
Nausea 5.6%
Disc. AE
120 mg 1 times / day multiple, oral
MTD
Dose: 120 mg, 1 times / day
Route: oral
Route: multiple
Dose: 120 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 18
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 18
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
Vomiting 5.6%
Disc. AE
120 mg 1 times / day multiple, oral
MTD
Dose: 120 mg, 1 times / day
Route: oral
Route: multiple
Dose: 120 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 18
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 18
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
Elevated triglycerides 12.5%
DLT
150 mg 1 times / day multiple, oral
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 8
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
Methemoglobinemia 12.5%
DLT, Disc. AE
150 mg 1 times / day multiple, oral
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 8
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
Fever 12.5%
Disc. AE
150 mg 1 times / day multiple, oral
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 8
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
Flushing 12.5%
Disc. AE
150 mg 1 times / day multiple, oral
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 8
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
Histoplasmosis 12.5%
Disc. AE
150 mg 1 times / day multiple, oral
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 8
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
Skin rash 12.5%
Disc. AE
150 mg 1 times / day multiple, oral
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 8
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
Methemoglobinemia 37.5%
DLT
150 mg 1 times / day multiple, oral
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
unhealthy, ADULT
n = 8
Health Status: unhealthy
Condition: HIV infection
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/10235511
Page: p.29
Acute renal failure 3.6%
Disc. AE
2.5 mg/kg 1 times / day multiple, oral
Studied dose
Dose: 2.5 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16354802
Page: p.1008
unhealthy, CHILD,ADULT
n = 28
Health Status: unhealthy
Condition: visceral leishmaniasis
Age Group: CHILD,ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 28
Sources:
https://pubmed.ncbi.nlm.nih.gov/16354802
Page: p.1008
Bone marrow depression 3.6%
Disc. AE
2.5 mg/kg 1 times / day multiple, oral
Studied dose
Dose: 2.5 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16354802
Page: p.1008
unhealthy, CHILD,ADULT
n = 28
Health Status: unhealthy
Condition: visceral leishmaniasis
Age Group: CHILD,ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 28
Sources:
https://pubmed.ncbi.nlm.nih.gov/16354802
Page: p.1008
Bone marrow depression 3.6%
Disc. AE
2.5 mg/kg 1 times / day multiple, oral
Studied dose
Dose: 2.5 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16354802
Page: p.1008
unhealthy, CHILD,ADULT
n = 28
Health Status: unhealthy
Condition: visceral leishmaniasis
Age Group: CHILD,ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 28
Sources:
https://pubmed.ncbi.nlm.nih.gov/16354802
Page: p.1008
Glomerulonephritis 7.2%
Disc. AE
2.5 mg/kg 1 times / day multiple, oral
Studied dose
Dose: 2.5 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16354802
Page: p.1008
unhealthy, CHILD,ADULT
n = 28
Health Status: unhealthy
Condition: visceral leishmaniasis
Age Group: CHILD,ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 28
Sources:
https://pubmed.ncbi.nlm.nih.gov/16354802
Page: p.1008
Nephrotic syndrome 7.2%
Disc. AE
2.5 mg/kg 1 times / day multiple, oral
Studied dose
Dose: 2.5 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16354802
Page: p.1008
unhealthy, CHILD,ADULT
n = 28
Health Status: unhealthy
Condition: visceral leishmaniasis
Age Group: CHILD,ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 28
Sources:
https://pubmed.ncbi.nlm.nih.gov/16354802
Page: p.1008
Cardio-respiratory failure grade 5, 3.6%
Disc. AE
2.5 mg/kg 1 times / day multiple, oral
Studied dose
Dose: 2.5 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/16354802
Page: p.1008
unhealthy, CHILD,ADULT
n = 28
Health Status: unhealthy
Condition: visceral leishmaniasis
Age Group: CHILD,ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 28
Sources:
https://pubmed.ncbi.nlm.nih.gov/16354802
Page: p.1008
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer
P-gp
1461
CYPs
33
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
P-gp
1650
 inconclusive [IC50 23.1093 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYPs
33
 yes
PubMed

PubMed

TitleDatePubMed
8-Aminoquinolines from Walter Reed Army Institute for Research for treatment and prophylaxis of Pneumocystis pneumonia in rat models.
1991 Feb
New drug developments for opportunistic infections in immunosuppressed patients: Pneumocystis carinii.
1995 Nov 24
Transition metal complexes of quinolino[3,2-b]benzodiazepine and quinolino[3,2-b]benzoxazepine: synthesis, characterization, and antimicrobial studies.
2007
Patents

Patents

20060172956
2
6316502
2
7927613
118
WO2011033115A2
2

Sample Use Guides

In Vivo Use Guide
oral sitamaquine, 2 mg/kg/day, once a day for 21 days
Route of Administration: Oral
In Vitro Use Guide
Sitamaquine (1 ug/ml) almost completely inhibited P carinii growth in human lung fibroblasts over 10 days. Some inhibition was seen at 0.1 ug/ml, which was a similar level of activity to that of primaquine.
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:33:06 GMT 2023
Edited
by admin
on Fri Dec 15 15:33:06 GMT 2023
Record UNII
ASU02O7NS8
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SITAMAQUINE DIHYDROCHLORIDE
MI  
Common Name English
1,6-HEXANEDIAMINE, N1,N1-DIETHYL-N6-(6-METHOXY-4-METHYL-8-QUINOLINYL)-, HYDROCHLORIDE (1:2)
Systematic Name English
NSC-2452
Code English
SITAMAQUINE DIHYDROCHLORIDE [MI]
Common Name English
N1,N1-DIETHYL-N6-(6-METHOXY-4-METHYL-8-QUINOLINYL)-1,6-HEXANEDIAMINE DIHYDROCHLORIDE
Systematic Name English
WR-6026
Code English
WR-6026 DIHYDROCHLORIDE
Code English
Code System Code Type Description
CAS
5330-29-0
Created by admin on Fri Dec 15 15:33:06 GMT 2023 , Edited by admin on Fri Dec 15 15:33:06 GMT 2023
PRIMARY
FDA UNII
ASU02O7NS8
Created by admin on Fri Dec 15 15:33:06 GMT 2023 , Edited by admin on Fri Dec 15 15:33:06 GMT 2023
PRIMARY
PUBCHEM
73340
Created by admin on Fri Dec 15 15:33:06 GMT 2023 , Edited by admin on Fri Dec 15 15:33:06 GMT 2023
PRIMARY
EPA CompTox
DTXSID80967884
Created by admin on Fri Dec 15 15:33:06 GMT 2023 , Edited by admin on Fri Dec 15 15:33:06 GMT 2023
PRIMARY
ECHA (EC/EINECS)
226-224-0
Created by admin on Fri Dec 15 15:33:06 GMT 2023 , Edited by admin on Fri Dec 15 15:33:06 GMT 2023
PRIMARY
MERCK INDEX
m9961
Created by admin on Fri Dec 15 15:33:06 GMT 2023 , Edited by admin on Fri Dec 15 15:33:06 GMT 2023
PRIMARY Merck Index
NSC
2452
Created by admin on Fri Dec 15 15:33:06 GMT 2023 , Edited by admin on Fri Dec 15 15:33:06 GMT 2023
PRIMARY
Related Record Type Details
Structure of SITAMAQUINE
PARENT -> SALT/SOLVATE
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