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CG5503 IR; tapentadol
Tapentadol is a mu-opioid receptor agonist and norepinephrine reuptake inhibitor that provides analgesia through dual mechanisms of action.
Tapentadol is a mu-opioid receptor agonist and norepinephrine reuptake inhibitor that provides analgesia through dual mechanisms of action. Used for Acute pain management, Moderate to severe pain.
At a glance
| Generic name | CG5503 IR; tapentadol |
|---|---|
| Sponsor | Johnson & Johnson Pharmaceutical Research & Development, L.L.C. |
| Drug class | Mu-opioid receptor agonist and norepinephrine reuptake inhibitor |
| Target | Mu-opioid receptor (OPRM1); norepinephrine transporter (SLC6A2) |
| Modality | Small molecule |
| Therapeutic area | Pain Management |
| Phase | Phase 3 |
Mechanism of action
Tapentadol binds to mu-opioid receptors in the central nervous system to produce opioid-mediated analgesia, while simultaneously inhibiting the reuptake of norepinephrine, which enhances descending pain inhibitory pathways. This dual mechanism allows for effective pain relief with a potentially lower side effect profile compared to traditional opioids. CG5503 IR is an immediate-release formulation of tapentadol.
Approved indications
- Acute pain management
- Moderate to severe pain
Common side effects
- Nausea
- Dizziness
- Somnolence
- Vomiting
- Constipation
- Headache
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 |
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