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Tizanidine · 1 trial · 1 indication
| Arm | Type | Description |
|---|---|---|
| Pharmacokinetic Population | EXPERIMENTAL | All participants will receive a 3-period treatment including single-dose tizanidine on Day 1, twice-daily vemurafenib on Days 2 to 21, and both agents together on Day 22. |
| Name | Type | Description |
|---|---|---|
| Tizanidine | DRUG | Participants will receive tizanidine as single oral doses, 2 milligrams (mg) on Day 1 and repeated on Day 22, each following an overnight fast \>/= 10 hours. |
| Vemurafenib | DRUG | Participants will receive vemurafenib as multiple oral doses, 960 mg twice daily on Days 2 to 22. |
Inclusion Criteria: * Adults 18 to 70 years of age, inclusive * Unresectable Stage IIIc or IV metastatic melanoma positive for the BRAFV600 mutation or other malignant tumor type which harbors a V600 activating mutation of BRAF, as determined by Cobas 4800 BRAFV600 Mutation Test or a DNA sequencing...
Tizanidine is being studied in oncology, specifically in patients with BRAFV600 mutation-positive metastatic malignancies including malignant melanoma and other neoplasms. It was evaluated in a Phase 1 drug interaction study, not as a stand-alone anticancer therapy. Tizanidine is a small molecule and is not approved for these cancer indications.
Tizanidine targets the alpha-2 adrenergic receptors ADRA2A, ADRA2B, and ADRA2C, where it acts as an agonist. These receptors are involved in regulating neurotransmitter release. In the oncology setting, Tizanidine was used as a probe to assess drug-drug interactions rather than to directly treat the tumor.
Roche Holding AG, which trades under the ticker RHHBY, is the developer associated with the oncology study of Tizanidine. The trial was sponsored to investigate the effect of vemurafenib on Tizanidine pharmacokinetics in patients with BRAFV600 mutation-positive metastatic malignancies.
Tizanidine is in Phase 1 development for malignant melanoma and neoplasms. The single Phase 1 trial has been completed, and no active trials are ongoing. Tizanidine is investigational for these cancer indications and has not been approved for them.
Tizanidine was evaluated in one completed Phase 1 trial, NCT01844674, titled A Study on the Effect of Vemurafenib on the Pharmacokinetics of a Single Dose of Tizanidine in Patients With BRAFV600 Mutation-Positive Metastatic Malignancies. The trial enrolled 18 patients across the United States, Brazil, Canada, Cyprus, and South Korea.
Tizanidine is also known by the brand name Zanaflex. In this oncology context, Tizanidine was used as a probe drug in a pharmacokinetic interaction study with vemurafenib, not as a primary treatment for melanoma or other neoplasms.