Evidence & regulatory context
- Mechanism
- Mu opioid receptor agonist; Norepinephrine transporter inhibitor
- Target
- CHEMBL233; CHEMBL222
- Injury models
- Other
- Reported indication
- Management of moderate-to-severe acute pain (and chronic/neuropathic pain) (approved 2008)
- First approval
- 2008
- Development stage
- Approved for acute (post-surgical/injury) pain, but with opioid abuse/respiratory-depression boxed warning
- ChEMBL max phase
- 4 / 4 (development scale, not regulatory approval)
- Synonyms
- BN-200; BN 200 (BASE); CG-5503; CG5503; CG5503 (BASE); CG5503 IR; NSC-759619; Tapentadol
- Note
- Not recorded
Clinical trials 9
0 linked trials carry an injury-indication flag. These flags support record-level exploration and sit alongside the stringent aggregate counts described in Methods.
Evaluation of Tapentadol PR Versus a Combination of Tapentadol PR and Pregabalin in Subjects With Severe Chronic Low Back Pain With a Neuropathic Pain Component
Low Back Pain · Neuropathic Pain
Enrolment: 622 · Results not recorded
Phase III Trial to Evaluate the Efficacy and Safety of CG5503 Extended-Release in Patients With Moderate to Severe Chronic Pain Due to Osteoarthritis of the Knee
Osteoarthritis, Knee · Pain
Enrolment: 1030 · Results not recorded
A Study of NUCYNTA (Tapentadol) Immediate Release vs. Oxycodone Immediate Release for the Treatment of Acute Low Back Pain
Pain · Back Pain · Low Back Pain · Back Pain With Radiation
Enrolment: 667 · Results not recorded
Study of Tapentadol IR for the Treatment of Acute Pain Caused by Vertebral Compression Fractures Associated With Osteoporosis
Back Pain
Enrolment: 108 · Results not recorded
Evaluation of the Population Pharmacokinetic Profile, Safety, Tolerability, and Efficacy of Tapentadol Oral Solution for Post-surgical Pain in Children Aged Birth to Less Than 2 Years
Moderate to Severe Acute Postoperative Pain
Enrolment: 40 · Results not recorded
Observational Study to Determine the Long-term Tolerability and Analgesic Effectiveness of Oral Tapentadol in Patients With Severe Pain Syndromes
Severe Pain Syndromes
Enrolment: 55 · Results not recorded
Post-Marketing Surveillance Study on the Safety and Effectiveness of Immediate Release Tapentadol Hydrochloride Among Adult Filipino Patients
Moderate to Severe Acute Non-Cancer Pain
Enrolment: 0 · Results not recorded
Prospective Longitudinal Observational Study to Evaluate the Clinical Characteristics and Opioids Treatments in Patients With Breakthrough Cancer Pain
Tumor · Cancer Pain · Breakthrough Cancer Pain · Neuropathic Pain
Enrolment: 150 · Results not recorded
Post-Marketing Surveillance Study on the Safety and Effectiveness of Prolonged Release Tapentadol Hydrochloride Among Adult Filipino Patients
Moderate to Severe Chronic Non-cancer Pain
Enrolment: 0 · Results not recorded
Preclinical evidence 1
1 studies reported at therapy level; 1 evidence entries itemised.
RatOtherSprague-DawleyMaleIntraperitoneal1 to 10 mg/kgTreatment 2 weeks after nerve constriction surgery
Model: Unilateral chronic constriction injury of the infraorbital nerve or of the sciatic nerve
Acute tapentadol significantly reduced allodynia after both infraorbital and sciatic nerve constriction, its anti-allodynic effect was maintained after 4 days of repeated treatment whereas the effect of morphine vanished, and treatment did not alter nerve lesion-evoked overexpression of activating…
Extraction: extract · Supplied extraction confidence: 0.8. Machine-extracted fields require source verification.
