Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C17H9Cl2FN4O2 |
| Molecular Weight | 391.183 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
FC1=CC=C(C=C1)C(C#N)C2=C(Cl)C=C(C=C2Cl)N3N=CC(=O)NC3=O
InChI
InChIKey=XQKYUBTUOHHNDV-UHFFFAOYSA-N
InChI=1S/C17H9Cl2FN4O2/c18-13-5-11(24-17(26)23-15(25)8-22-24)6-14(19)16(13)12(7-21)9-1-3-10(20)4-2-9/h1-6,8,12H,(H,23,25,26)
| Molecular Formula | C17H9Cl2FN4O2 |
| Molecular Weight | 391.183 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
Letrazuril is the p-fluoro analogue of diclazuril, a benzeneacetonitrile which is active against Eimeria spp., the causative agent of coccidiosis in poultry. Letrazuril is better absorbed and unlike diclazuril produces detectable plasma drug levels in humans following oral administration. In experimental studies on neonatal mice infected with Cryptosporidium parvum, oral administration of letrazuril for 4 days reduced stool oocyst counts by 95-98%, with complete clearing of oocysts from the stool in 47% of animals receiving the higher dose. Letrazuril has the potential to be an effective agent in the treatment of AIDS-related Cryptosporidiosis, without associated major toxicity. Severely immunocompromised AIDS patients with refractory cryptosporidiosis may show a modest, short-lived response to letrazuril. Letrazuril had been in phase I clinical trials for the treatment of cryptosporidiosis. However, this study was discontinued.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Pilot studies of azithromycin, letrazuril and paromomycin in the treatment of cryptosporidiosis. | 1997-02 |
|
| Treatment with letrazuril of refractory cryptosporidial diarrhea complicating AIDS. | 1995-09-01 |
|
| A phase I study of letrazuril in AIDS-related cryptosporidiosis. | 1994-08 |
|
| Successful treatment of AIDS-related cryptosporidial sclerosing cholangitis. | 1993-11 |
|
| Successful treatment of cryptosporidiosis in an AIDS patient with letrazuril. | 1993-09 |
|
| Letrazuril therapy for cryptosporidiosis: clinical response and pharmacokinetics. | 1993-03 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7986407
50 to 100 mg daily for 6 weeks
Route of Administration:
Oral
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 19:17:19 GMT 2025
by
admin
on
Mon Mar 31 19:17:19 GMT 2025
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| Record UNII |
U8736VCB22
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| Record Status |
Validated (UNII)
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