Fidaxomicin

Summary

Fidaxomicin (CHEMBL1255800) is an approved small molecule (ATC A07AA12); indicated across 4 conditions including diarrheal disease and clostridium infectious disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A07AA12
• Indications: 4 conditions
• Clinical trials: 29
• Chemistry: 1058 Da · C52H74Cl2O18

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1255800
Name	Fidaxomicin
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	10034073
ATC	A07AA12
Molecular formula	C52H74Cl2O18
Molecular weight	1058
InChIKey	ZVGNESXIJDCBKN-UUEYKCAUSA-N

SMILES: CC[C@H]1/C=C(/[C@H](C/C=C/C=C(/C(=O)O[C@@H](C/C=C(/C=C(/[C@@H]1O[C@H]2[C@H]([C@H]([C@@H](C(O2)(C)C)OC(=O)C(C)C)O)O)\C)\C)[C@@H](C)O)\CO[C@H]3[C@H]([C@H]([C@@H]([C@H](O3)C)OC(=O)C4=C(C(=C(C(=C4O)Cl)O)Cl)CC)O)OC)O)\C

IUPAC name: [(2R,3S,4S,5S,6R)-6-[[(3E,5E,8S,9E,11S,12R,13E,15E,18S)-12-[(2R,3S,4R,5S)-3,4-dihydroxy-6,6-dimethyl-5-(2-methylpropanoyloxy)oxan-2-yl]oxy-11-ethyl-8-hydroxy-18-[(1R)-1-hydroxyethyl]-9,13,15-trimethyl-2-oxo-1-oxacyclooctadeca-3,5,9,13,15-pentaen-3-yl]methoxy]-4-hydroxy-5-methoxy-2-methyloxan-3-yl] 3,5-dichloro-2-ethyl-4,6-dihydroxybenzoate

Also known as: Dificid, Dificlir, Fidaxomicin, Fidaxomicina, Fidaxomicine, OPT-80, PAR-101, fidaxomicin, FIDAXOMICIN, Tiacumicin B; Fidaxomicin

Patent coverage: 892 distinct patent families (2,010 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,954 (97%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 8 (assay-derived). Sample: Equilibrative nucleoside transporter 1, Progesterone receptor, 5-hydroxytryptamine receptor 2A, Prostaglandin G/H synthase 2, Substance-P receptor, Adenosine receptor A3, Gastrin/cholecystokinin type B receptor, Androgen receptor.

Bioactivity

ChEMBL activities: 3 potent at pChembl ≥ 5 of 9 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SLC29A1	5.44	AC50	3600	nM	CHEMBL_ACT_25141465
TACR1	5.23	AC50	5920	nM	CHEMBL_ACT_25128733
CCKBR	5.1	AC50	7900	nM	CHEMBL_ACT_25171392

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

4 indications (4 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
diarrheal disease	4	MONDO:0001673	HP:0002014
Clostridium infectious disease	4	MONDO:0024388	EFO:1000874

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 29.

Phase distribution

Phase	Trials
PHASE4	11
PHASE3	9
PHASE2	4
Not specified	3
PHASE1	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06794944	PHASE4	NOT_YET_RECRUITING	Use of Fidaxomicin Compared to Vancomycin for Decolonization of C. Difficile in Patients With Inflammatory Bowel Disease
NCT01552668	PHASE4	WITHDRAWN	Fidaxomicin to Prevent Clostridium Difficile Colonization
NCT01775397	PHASE4	TERMINATED	A Post-marketing, Blinded Study to Investigate How Effective Fidaxomicin is Compared to Vancomycin in the Sustained Cure of Clostridium Difficile Infection in Adults That Are Receiving Therapy to Suppress the Immune System
NCT01818141	PHASE4	COMPLETED	Study to Assess Inhibition of Spore Production in Patients With C. Difficile Infections: Fidaxomicin Versus Vancomycin
NCT02057198	PHASE4	COMPLETED	Impact of Oral Antibiotic Treatment on C. Difficile
NCT02254967	PHASE4	COMPLETED	A Phase IIIB/IV Study to Compare the Efficacy of Vancomycin Therapy to Extended Duration of Fidaxomicin Therapy in the Clinical Cure of Clostridium Difficile Infection (CDI) in an Older Population
NCT02355938	PHASE4	TERMINATED	Use Of Oral Fidaxomicin Vs. Oral Vancomycin For Clostridium Difficile Infection In Patients With Spinal Cord Injury
NCT02437591	PHASE4	COMPLETED	Study to Evaluate the Pharmacokinetics of Fidaxomicin in Inflammatory Bowel Disease (IBD) Subjects With Clostridium Difficile Infection (CDI)
NCT02464306	PHASE4	WITHDRAWN	Fidaxomicin Versus Standard of Care Therapy in Solid Organ Transplant Recipients With Clostridium Difficile Infection
NCT02667418	PHASE4	TERMINATED	Optimal Treatment for Recurrent Clostridium Difficile
NCT02692651	PHASE4	COMPLETED	A Comparison of Fidaxomicin and Vancomycin in Patients With CDI Receiving Antibiotics for Concurrent Infections
NCT07328971	PHASE3	RECRUITING	Vancomycin Taper to Prevent Recurrent Clostridioides Difficile
NCT00314951	PHASE3	COMPLETED	Fidaxomicin Versus Vancomycin for the Treatment of Clostridium Difficile-Associated Diarrhea (CDAD) (MK-5119-018)
NCT00468728	PHASE3	COMPLETED	PAR-101/OPT-80 Versus Vancomycin for the Treatment of Clostridium Difficile-Associated Diarrhea (CDAD)
NCT01691248	PHASE3	COMPLETED	Safety and Efficacy of Fidaxomicin Versus Placebo for Prophylaxis Against Clostridium Difficile-Associated Diarrhea in Adults Undergoing Hematopoietic Stem Cell Transplantation (MK-5119-001)
NCT02179658	PHASE3	COMPLETED	A Study to Compare Safety and Efficacy of OPT-80(Fidaxomicin) With Vancomycin in Subjects With Clostridium Difficile-associated Diarrhea (CDAD)
NCT02218372	PHASE3	COMPLETED	A Study to Investigate the Safety and Efficacy of Fidaxomicin (Oral Suspension or Tablets) and Vancomycin (Oral Liquid or Capsules) in Pediatric Subjects With Clostridium Difficile-associated Diarrhea (CDAD)
NCT02395848	PHASE3	TERMINATED	Efficacy of 30-day Duration of Fidaxomicin for Recurrent C. Difficile Infection
NCT02743234	PHASE3	COMPLETED	Fecal Microbiota Transplantation for Relapsing Clostridium Difficile Infection
NCT05201079	PHASE3	COMPLETED	Primary or Recurrent Clostridioides Difficile Infection Treatment With Capsules of Lyophilised Faecal Microbiota vs Fidaxomicin
NCT00097422	PHASE2	COMPLETED	OPT-80 in Clostridium Difficile-Associated Diarrhea (CDAD)
NCT01591863	PHASE2	COMPLETED	Safety, Tolerability, and Pharmacokinetics of Fidaxomicin in Pediatric Subjects With Clostridium Difficile-associated Diarrhea (CDAD)
NCT02784002	PHASE2	COMPLETED	A Study of Ridinilazole (SMT19969) Compared With Fidaxomicin for the Treatment of Clostridium Difficile Infection (CDI)
NCT03760484	PHASE2	TERMINATED	Fecal Microbiota Transplant (FMT) Plus Fidaxomicin for Severe or Fulminant Clostridium Difficile Infection
NCT01813448	PHASE1	COMPLETED	A Study to Assess the Safety, Tolerability and Pharmacokinetics of Single and Multiple Ascending Doses of Fidaxomicin in Healthy Male Japanese and Caucasian Subjects
NCT02083627	PHASE1	COMPLETED	A Study to Assess the Effects of Multiple Doses of Fidaxomicin on a Single Dose of Rosuvastatin in Healthy Male Subjects
NCT07120490	Not specified	NOT_YET_RECRUITING	STOP-CDI: Efficacy of Fecal Microbiota Transplantation vs Fidaxomicin vs Vancomycin in Treating and Preventing Relapse of Clostridioides Difficile Infection
NCT02214771	Not specified	COMPLETED	Description of the Use of fidAxomicin in Hospitalized Patients With Documented Clostridium diFficile iNfection and of the managEment of These Patients
NCT04070352	Not specified	WITHDRAWN	Evaluation of Fidaxomicin in the Treatment of Clostridium Difficile Infection (CDI)

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).