cadazolid
Cadazolid is an experimental antibiotic of the oxazolidinone class made by Actelion Pharmaceuticals Ltd. which is effective against Clostridioides difficile, a major cause of drug resistant diarrhea in the elderly. Current drug treatments for this infection involve orally delivered antibiotics, principally fidaxomicin, metronidazole and vancomycin; the last two drugs are the principal therapeutic agents in use, but fail in approximately 20 to 45% of the cases. The drug works by inhibiting the synthesis of proteins in the bacteria, thus inhibiting the production of toxins and the formation of spores. Cadazolid progressed through to Phase III clinical trials, but in its financial results for Q1 2018, Idorsia mentions that Actelion informed them that "following completion of Phase 3 data analysis of cadazolid - it has decided to discontinue the development of the compound." — Wikipedia
Clinical trial activity
4 trials · 1 clinical orgs · 0 marketing orgs
Earliest trial started Jan 25, 2011 (NCT01222702)
Timeline
Indications
Studied for
Mechanism of action
- Bacterial 70S ribosomeINHIBITOR
Bacterial 70S ribosome inhibitor
23S RNA
- 30S ribosomal protein S2 (rpsB) ↗
- 50S ribosomal protein L4 (rplD) ↗
- 30S ribosomal protein S15 (rpsO) ↗
- 30S ribosomal protein S16 (rpsP) ↗
- 30S ribosomal protein S17 (rpsQ) ↗
- 30S ribosomal protein S18 (rpsR) ↗
- 30S ribosomal protein S19 (rpsS) ↗
- 30S ribosomal protein S20 (rpsT) ↗
- 30S ribosomal protein S21 (rpsU) ↗
- 30S ribosomal protein S3 (rpsC) ↗
- 30S ribosomal protein S4 (rpsD) ↗
- 30S ribosomal protein S5 (rpsE) ↗
- 30S ribosomal protein S6 (rpsF) ↗
- 30S ribosomal protein S7 (rpsG) ↗
- 30S ribosomal protein S8 (rpsH) ↗
- 30S ribosomal protein S9 (rpsI) ↗
- 50S ribosomal protein L35 (rpmI) ↗
- 50S ribosomal protein L36 2 (ykgO) ↗
- 50S ribosomal protein L36 (rpmJ) ↗
- 50S ribosomal protein L3 (rplC) ↗
- 50S ribosomal protein L5 (rplE) ↗
- 50S ribosomal protein L6 (rplF) ↗
- 50S ribosomal protein L7/L12 (rplL) ↗
- 30S ribosomal protein S1 (rpsA) ↗
- 30S ribosomal protein S10 (rpsJ) ↗
- 30S ribosomal protein S11 (rpsK) ↗
- 30S ribosomal protein S12 (rpsL) ↗
- 30S ribosomal protein S13 (rpsM) ↗
- 30S ribosomal protein S14 (rpsN) ↗
- 50S ribosomal protein L10 (rplJ) ↗
- 50S ribosomal protein L11 (rplK) ↗
- 50S ribosomal protein L13 (rplM) ↗
- 50S ribosomal protein L14 (rplN) ↗
- 50S ribosomal protein L15 (rplO) ↗
- 50S ribosomal protein L16 (rplP) ↗
- 50S ribosomal protein L17 (rplQ) ↗
- 50S ribosomal protein L18 (rplR) ↗
- 50S ribosomal protein L19 (rplS) ↗
- 50S ribosomal protein L1 (rplA) ↗
- 50S ribosomal protein L20 (rplT) ↗
- 50S ribosomal protein L21 (rplU) ↗
- 50S ribosomal protein L22 (rplV) ↗
- 50S ribosomal protein L23 (rplW) ↗
- 50S ribosomal protein L24 (rplX) ↗
- 50S ribosomal protein L25 (rplY) ↗
- 50S ribosomal protein L27 (rpmA) ↗
- 50S ribosomal protein L28 (rpmB) ↗
- 50S ribosomal protein L29 (rpmC) ↗
- 50S ribosomal protein L2 (rplB) ↗
- 50S ribosomal protein L30 (rpmD) ↗
- 50S ribosomal protein L31 type B (ykgM) ↗
- 50S ribosomal protein L31 (rpmE) ↗
- 50S ribosomal protein L32 (rpmF) ↗
- 50S ribosomal protein L33 (rpmG) ↗
- 50S ribosomal protein L34 (rpmH) ↗
Chemistry & pharmacology
SMILES
O=C(O)c1cn(C2CC2)c2cc(N3CCC(O)(COc4ccc(N5C[C@H](CO)OC5=O)cc4F)CC3)c(F)cc2c1=O- Mol. weight
- 585.56 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaCadazolid ↗
- ChEMBLCHEMBL3707376 ↗
Also known as
- act-179811
- act-179811
- cadazolid
- cadazolid
- cadazolid
- cadazolid
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT01987895 | Phase 3 | Mar 27, 2014 | Actelion |
| NCT01983683 | Phase 3 | Dec 12, 2013 | Actelion |
| NCT02053181 | Phase 1 | Aug 1, 2012 | Actelion |
| NCT01222702 | Phase 2 | Jan 25, 2011 | Actelion |
Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Actelion | For profit | 4 | 4 | 3 | 2011 |