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Rectal tacrolimus
Tacrolimus suppresses local immune responses in the rectum by inhibiting calcineurin and reducing T-cell activation, helping to control inflammatory bowel disease.
Tacrolimus suppresses local immune responses in the rectum by inhibiting calcineurin and reducing T-cell activation, helping to control inflammatory bowel disease. Used for Ulcerative colitis (rectal/distal disease), Inflammatory bowel disease (IBD).
At a glance
| Generic name | Rectal tacrolimus |
|---|---|
| Also known as | calcineurin inhibitor |
| Sponsor | The University of Western Australia |
| Drug class | Calcineurin inhibitor |
| Target | Calcineurin (protein phosphatase 2B) |
| Modality | Small molecule |
| Therapeutic area | Gastroenterology / Immunology |
| Phase | FDA-approved |
Mechanism of action
Tacrolimus is a calcineurin inhibitor that blocks T-cell proliferation and cytokine production by preventing dephosphorylation of nuclear factor of activated T cells (NFAT). When administered rectally, it delivers high local concentrations to inflamed colonic tissue while minimizing systemic exposure, making it suitable for treating distal inflammatory bowel conditions.
Approved indications
- Ulcerative colitis (rectal/distal disease)
- Inflammatory bowel disease (IBD)
Common side effects
- Local rectal irritation
- Headache
- Abdominal discomfort
- Systemic immunosuppression (if absorbed)
Key clinical trials
- Rectal Indomethacin and Oral Tacrolimus Versus Combination to Prevent Post-ERCP Pancreatitis (PHASE3)
- Tacrolimus Lipid Suspension for Enema in Adult Subjects with Mild to Moderately Active Left-sided/Distal Ulcerative Colitis Who Had an Inadequate Response to the Treatment (PHASE2)
- Medical Treatment of Colitis in Patients With Hermansky-Pudlak Syndrome (PHASE2)
- Rectal Tacrolimus in the Treatment of Resistant Ulcerative Proctitis (PHASE4)
- Pharmacokinetic Study to Rectal and Sublingual Administration of Tacrolimus in Future Kidney Transplant Patients (PHASE1)
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 |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Rectal tacrolimus CI brief — competitive landscape report
- Rectal tacrolimus updates RSS · CI watch RSS
- The University of Western Australia portfolio CI