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Mytesi (CROFELEMER)
Mytesi works by blocking the action of a specific protein called anoctamin-1, which helps regulate the movement of water and electrolytes in the intestines.
Mytesi (CROFELEMER) is a small molecule antidiarrheal medication originally developed by Salix Pharmaceuticals and currently owned by Napo Pharmaceuticals Inc. It targets the anoctamin-1 receptor to treat non-infectious diarrhea. Mytesi is a patented medication with no generic manufacturers available. It was FDA-approved in 2012 for its approved indications. Key safety considerations include the need for monitoring of liver function and potential interactions with other medications.
At a glance
| Generic name | CROFELEMER |
|---|---|
| Sponsor | Napo Pharms Inc |
| Drug class | Antidiarrheal [EPC] |
| Target | Anoctamin-1 |
| Modality | Small molecule |
| Therapeutic area | Infectious Disease |
| Phase | FDA-approved |
| First approval | 2012 |
Mechanism of action
Crofelemer is an inhibitor of both the cyclic adenosine monophosphate (cAMP)-stimulated cystic fibrosis transmembrane conductance regulator (CFTR) chloride ion (Cl) channel, and the calcium-activated Cl channels (CaCC) at the luminal membrane of enterocytes. The CFTR Cl channel and CaCC regulate Cl and fluid secretion by intestinal epithelial cells. Crofelemer acts by blocking Cl secretion and accompanying high volume water loss in diarrhea, normalizing the flow of Cl and water in the gastrointestinal tract.
Approved indications
- Non-infective diarrhea
Common side effects
- Upper respiratory tract infection
- Bronchitis
- Cough
- Flatulence
- Increased bilirubin
- Nausea
- Back pain
- Arthralgia
- Urinary tract infection
- Nasopharyngitis
- Musculoskeletal pain
- Hemorrhoids
Key clinical trials
- Crofelemer for Functional Diarrhea (PHASE4)
- Yield of Diagnostic Tests and Effects of Crofelemer for Chronic Idiopathic Diarrhea In Non-HIV Patients (PHASE4)
- Open-Label Pilot Study With Crofelemer in Patients With Short Bowel Syndrome (EARLY_PHASE1)
- Incidence and Severity of Diarrhea in Patients With HER2 Positive Breast Cancer Treated With Trastuzumab and Neratinib (PHASE2)
- Ascending Doses of Crofelemer Powder for Oral Solution in Pediatric Microvillus Inclusion Disease (MVID) (PHASE2)
- Safety and Efficacy of Crofelemer in Adult Patients With Short Bowel Syndrome and Intestinal Failure (SBS-IF) Without Colon-in-continuity (CIC) (PHASE2)
- Prophylaxis of Diarrhea in Adult Cancer Patients Receiving Targeted Cancer Therapy (PHASE3)
- Diarrhea Prevention and Prophylaxis With Crofelemer in HER2 Positive Breast Cancer Patients (PHASE2)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Mytesi CI brief — competitive landscape report
- Mytesi updates RSS · CI watch RSS
- Napo Pharms Inc portfolio CI