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CG5503 IR
CG5503 is a selective inhibitor of transient receptor potential vanilloid 1 (TRPV1) that reduces pain signaling by blocking capsaicin-sensitive nociceptors.
CG5503 is a selective inhibitor of transient receptor potential vanilloid 1 (TRPV1) that reduces pain signaling by blocking capsaicin-sensitive nociceptors. Used for Chronic pain conditions (Phase 3 development).
At a glance
| Generic name | CG5503 IR |
|---|---|
| Also known as | Tapentadol |
| Sponsor | Grünenthal GmbH |
| Drug class | TRPV1 antagonist |
| Target | TRPV1 (Transient Receptor Potential Vanilloid 1) |
| Modality | Small molecule |
| Therapeutic area | Pain Management |
| Phase | Phase 3 |
Mechanism of action
TRPV1 is a cation channel expressed on sensory neurons that mediates pain, heat, and inflammatory responses. By selectively antagonizing TRPV1, CG5503 reduces the transmission of pain signals from peripheral nociceptors to the central nervous system. This mechanism is intended to provide analgesia while potentially minimizing systemic side effects associated with non-selective pain therapeutics.
Approved indications
- Chronic pain conditions (Phase 3 development)
Common side effects
- Hyperthermia or impaired thermoregulation
- Gastrointestinal effects
- Peripheral edema
Key clinical trials
- Evaluation of the Antihyperalgesic Effect of Tapentadol in Two Human Experimental Models (PHASE1)
- A Study to Look at Tapentadol Oral Solution in Children and Adolescents in Pain (PHASE3)
- A Study to Evaluate the Efficacy and Safety of Tapentadol (CG5503) in the Treatment of Acute Pain After Abdominal Hysterectomy (PHASE3)
- Evaluation of Effectiveness and Tolerability of Tapentadol Hydrochloride in Subjects With Severe Pain Due to Osteoarthritis Taking Either WHO Step I or Step II Analgesics or no Regular Analgesic (PHASE3)
- Evaluation of Effectiveness and Tolerability of Tapentadol Hydrochloride in Subjects With Severe Pain Due to Osteoarthritis Taking WHO Step III Analgesics But Showing a Lack of Tolerability. (PHASE3)
- Drug-drug Interaction Study to Evaluate the Effect of Omeprazole on CG5503 (Tapentadol) (PHASE1)
- Evaluation of Effectiveness and Tolerability of Tapentadol Hydrochloride in Subjects With Severe Chronic Low Back Pain Taking Either WHO Step I or Step II Analgesics or no Regular Analgesics (PHASE3)
- A Safety and Effectiveness Study of Immediate Release Tapentadol Hydrochloride Among Filipino Patients With Moderate to Severe Acute Non-Cancer Pain
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:
- CG5503 IR CI brief — competitive landscape report
- CG5503 IR updates RSS · CI watch RSS
- Grünenthal GmbH portfolio CI