[CAS NO. 59729-37-2] Fexinidazole
PRODUCTS SPECIFICATIONS [59729-37-2]
DESCRIPTION [59729-37-2]
Overview
| MDL | MFCD00866607 |
|---|---|
| Molecular Weight | 279.31 |
| Molecular Formula | C12H13N3O3S |
| SMILES | O=[N+](C1=CN=C(COC2=CC=C(SC)C=C2)N1C)[O-] |
Summary
Fexinidazole (HOE 239) is an orally active, potent nitroimidazole antitrypanosomal drug. Fexinidazole shows trypanocidal activity against T. brucei subspecies and strains with IC 50 s of 0.7-3.3 μM (0.2-0.9 μg/ml). Fexinidazol has the potential for human sleeping sickness (HAT) caused by infection with T. brucei [1] .
In Vitro
Fexinidazole (HOE 239) has two principal metabolites, sulfoxide and sulfone. They have shown trypanocidal activity in vitro with IC
50
s of 0.7-3.3 μM (0.2-0.9 μg/ml) range against all parasite strains tested
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Fexinidazole (HOE 239; 20-50 mg/kg/day of IP or 25-100 mg/kg/day of PO; four consecutive days) has antitrypanosomal activities
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Adult female NMRI mice weighing between 20 and 25 g T. b. rhodesiense [1] |
| Dosage: | 20, 50 mg/kg (IP) or 25, 50, 100 mg/kg (PO) |
| Administration: | IP or PO; daily; four consecutive days |
| Result: | Had antitrypanosomal activities, with 100 mg/kg/day p.o. being 100% curative. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01980199 | Drugs for Neglected Diseases |
Visceral Leishmaniasis
|
November 2013 | Phase 2 |
| NCT01483170 | Drugs for Neglected Diseases |
Trypanosomiasis, African
|
September 2011 | Phase 1 |
| NCT03974178 | Drugs for Neglected Diseases|European and Developing Countries Clinical Trials Partnership (EDCTP) |
Trypanosoma Brucei Rhodesiense; Infection
|
September 29, 2019 | Phase 2|Phase 3 |
| NCT03025789 | Drugs for Neglected Diseases|Sanofi |
Trypanosomiasis, African|Sleeping Sickness|Trypanosomiasis; Gambian
|
November 17, 2016 | Phase 3 |
| NCT02498782 | Drugs for Neglected Diseases |
Chagas Disease|Trypanosomiasis, South American|South American Trypanosomiasis|Disease, Chagas
|
July 2014 | Phase 2 |
| NCT01340157 | Drugs for Neglected Diseases|Sanofi |
PK in Healthy Volunteers
|
February 2011 | Phase 1 |
| NCT02571062 | Drugs for Neglected Diseases |
Trypanosomiasis, African
|
March 2015 | Phase 1 |
| NCT05607173 | Sanofi |
Hepatic Function Abnormal
|
December 2022 | Phase 1 |
| NCT03587766 | Drugs for Neglected Diseases |
Chagas´ Disease (Chronic) Nos
|
November 13, 2017 | Phase 2 |
| NCT02184689 | Drugs for Neglected Diseases |
Human African Trypanosomiasis (HAT)
|
May 3, 2014 | Phase 2|Phase 3 |
| NCT01685827 | Drugs for Neglected Diseases |
Human African Trypanosomiasis (HAT)|Sleeping Sickness
|
October 2012 | Phase 2|Phase 3 |
| NCT02169557 | Drugs for Neglected Diseases |
Human African Trypanosomiasis (HAT)
|
April 30, 2014 | Phase 2|Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 179.01 mM ; Need ultrasonic)
H 2 O : < 0.1 mg/mL (insoluble)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.5803 mL | 17.9013 mL | 35.8025 mL |
| 5 mM | 0.7161 mL | 3.5803 mL | 7.1605 mL |
| 10 mM | 0.3580 mL | 1.7901 mL | 3.5803 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: 2.5 mg/mL (8.95 mM); Clear solution; Need warming
Synonyms