riluzole has been researched along with Malignant Melanoma in 15 studies
Riluzole: A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.
| Excerpt | Relevance | Reference |
|---|---|---|
| "Our data show that glutamate blockade with riluzole can inhibit signaling through the mitogen-activated protein kinase and phosphatidylinositol 3-kinase/AKT pathways and suppress the metabolic activity of melanoma." | 9.14 | A phase 0 trial of riluzole in patients with resectable stage III and IV melanoma. ( Chan, JL; Chen, S; Goydos, JS; Kempf, J; Le, MN; Lee, JH; Mehnert, JA; Shih, WJ; Yip, D; Yudd, A, 2009) |
| " Earlier, we demonstrated the accumulation of phosphorylated histone H2AX (γH2AX), a marker for DNA damage when mGluR1-expressing melanoma cells were treated with a functional inhibitor, riluzole." | 7.96 | Nonhomologous end-joining repair is likely involved in the repair of double-stranded DNA breaks induced by riluzole in melanoma cells. ( Cerchio, R; Chen, S; Foo, TK; Marinaro, C; Xia, B, 2020) |
| "Riluzole (1) is an approved therapeutic for the treatment of ALS and has also demonstrated anti-melanoma activity in metabotropic glutamate GRM1 positive cell lines, a mouse xenograft assay and human clinical trials." | 7.78 | Riluzole prodrugs for melanoma and ALS: design, synthesis, and in vitro metabolic profiling. ( Blass, BE; Chen, S; Fernandez-Metzler, C; King, RC; McDonnell, ME; Pelletier, JC; Reitz, AB; Smith, GR; Vera, MD; Wall, BA; Wrobel, J, 2012) |
| "Riluzole, an inhibitor of glutamate release, has shown the ability to inhibit melanoma cell xenograft growth." | 7.78 | Non-canonical Smads phosphorylation induced by the glutamate release inhibitor, riluzole, through GSK3 activation in melanoma. ( Abushahba, W; Boregowda, RK; Cohen-Solal, KA; Goydos, JS; Jeong, BS; Lasfar, A; Liu, F; Olabisi, OO; Wen, Y, 2012) |
| "Riluzole was well tolerated, with fatigue (62%) as the most common adverse event." | 6.87 | A phase II trial of riluzole, an antagonist of metabotropic glutamate receptor 1 (GRM1) signaling, in patients with advanced melanoma. ( Chen, S; Dudek, L; Goydos, JS; Jeong, BS; Kane, M; Lee, JH; Li, J; Lin, H; Mehnert, JM; Sadimin, E; Schenkel, JM; Shih, WJ; Silk, AW; Zloza, A, 2018) |
| "Current treatment for melanoma metastatic to the brain is grouped into those providing symptomatic relief such as corticosteroids and antiepileptic agents, to those that are disease modifying." | 6.52 | The current management of brain metastasis in melanoma: a focus on riluzole. ( Chen, S; Wall, BA; Yu, LJ, 2015) |
| " Treatment with riluzole, a glutamate release inhibitor, has been previously shown to be safe in melanoma patients and produced biologic effects, but did not lead to radiographic responses, possibly due to poor pharmacokinetic properties." | 5.51 | A phase Ib dose-escalation study of troriluzole (BHV-4157), an oral glutamatergic signaling modulator, in combination with nivolumab in patients with advanced solid tumors. ( Berman, RM; Chan, N; Chen, S; Coric, V; Girda, E; Groisberg, R; Malhotra, J; Mehnert, JM; Palmeri, M; Saraiya, B; Saunders, T; Shih, W; Silk, AW; Spencer, K; Vieth, J; Zloza, A, 2022) |
| "Riluzole-treated cells accumulate in G(2)/M phase of the cell cycle at 24 hours, and then undergo apoptotic cell death." | 5.37 | Riluzole enhances ionizing radiation-induced cytotoxicity in human melanoma cells that ectopically express metabotropic glutamate receptor 1 in vitro and in vivo. ( Ahlawat, S; Chen, S; Goydos, JS; Green, C; Haffty, BG; Khan, AJ; Mehnert, JM; Schiff, D; Wall, B, 2011) |
| "Our data show that glutamate blockade with riluzole can inhibit signaling through the mitogen-activated protein kinase and phosphatidylinositol 3-kinase/AKT pathways and suppress the metabolic activity of melanoma." | 5.14 | A phase 0 trial of riluzole in patients with resectable stage III and IV melanoma. ( Chan, JL; Chen, S; Goydos, JS; Kempf, J; Le, MN; Lee, JH; Mehnert, JA; Shih, WJ; Yip, D; Yudd, A, 2009) |
| " Earlier, we demonstrated the accumulation of phosphorylated histone H2AX (γH2AX), a marker for DNA damage when mGluR1-expressing melanoma cells were treated with a functional inhibitor, riluzole." | 3.96 | Nonhomologous end-joining repair is likely involved in the repair of double-stranded DNA breaks induced by riluzole in melanoma cells. ( Cerchio, R; Chen, S; Foo, TK; Marinaro, C; Xia, B, 2020) |
| "Riluzole (1) is an approved therapeutic for the treatment of ALS and has also demonstrated anti-melanoma activity in metabotropic glutamate GRM1 positive cell lines, a mouse xenograft assay and human clinical trials." | 3.78 | Riluzole prodrugs for melanoma and ALS: design, synthesis, and in vitro metabolic profiling. ( Blass, BE; Chen, S; Fernandez-Metzler, C; King, RC; McDonnell, ME; Pelletier, JC; Reitz, AB; Smith, GR; Vera, MD; Wall, BA; Wrobel, J, 2012) |
| "Riluzole, an inhibitor of glutamate release, has shown the ability to inhibit melanoma cell xenograft growth." | 3.78 | Non-canonical Smads phosphorylation induced by the glutamate release inhibitor, riluzole, through GSK3 activation in melanoma. ( Abushahba, W; Boregowda, RK; Cohen-Solal, KA; Goydos, JS; Jeong, BS; Lasfar, A; Liu, F; Olabisi, OO; Wen, Y, 2012) |
| "Melanoma cell lines that express GRM1 and either wild-type B-RAF or mutated B-RAF were treated with riluzole, sorafenib, PLX4720, or the combination of riluzole either with sorafenib or with PLX4720." | 3.77 | Glutamatergic pathway targeting in melanoma: single-agent and combinatorial therapies. ( Chan, JL; Chen, S; Goydos, JS; Lee, HJ; Namkoong, J; Rosenberg, S; Shin, SS; Wall, BA; Wangari-Talbot, J, 2011) |
| "Riluzole was well tolerated, with fatigue (62%) as the most common adverse event." | 2.87 | A phase II trial of riluzole, an antagonist of metabotropic glutamate receptor 1 (GRM1) signaling, in patients with advanced melanoma. ( Chen, S; Dudek, L; Goydos, JS; Jeong, BS; Kane, M; Lee, JH; Li, J; Lin, H; Mehnert, JM; Sadimin, E; Schenkel, JM; Shih, WJ; Silk, AW; Zloza, A, 2018) |
| "Current treatment for melanoma metastatic to the brain is grouped into those providing symptomatic relief such as corticosteroids and antiepileptic agents, to those that are disease modifying." | 2.52 | The current management of brain metastasis in melanoma: a focus on riluzole. ( Chen, S; Wall, BA; Yu, LJ, 2015) |
| "Riluzole-treated cells accumulate in G(2)/M phase of the cell cycle at 24 hours, and then undergo apoptotic cell death." | 1.37 | Riluzole enhances ionizing radiation-induced cytotoxicity in human melanoma cells that ectopically express metabotropic glutamate receptor 1 in vitro and in vivo. ( Ahlawat, S; Chen, S; Goydos, JS; Green, C; Haffty, BG; Khan, AJ; Mehnert, JM; Schiff, D; Wall, B, 2011) |
| Timeframe | Studies, this research(%) | All Research% |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (13.33) | 29.6817 |
| 2010's | 11 (73.33) | 24.3611 |
| 2020's | 2 (13.33) | 2.80 |
| Authors | Studies |
|---|---|
| McDonnell, ME | 1 |
| Vera, MD | 1 |
| Blass, BE | 1 |
| Pelletier, JC | 1 |
| King, RC | 1 |
| Fernandez-Metzler, C | 1 |
| Smith, GR | 1 |
| Wrobel, J | 1 |
| Chen, S | 13 |
| Wall, BA | 6 |
| Reitz, AB | 1 |
| Silk, AW | 2 |
| Saraiya, B | 1 |
| Groisberg, R | 1 |
| Chan, N | 1 |
| Spencer, K | 1 |
| Girda, E | 1 |
| Shih, W | 1 |
| Palmeri, M | 1 |
| Saunders, T | 1 |
| Berman, RM | 1 |
| Coric, V | 1 |
| Zloza, A | 2 |
| Vieth, J | 1 |
| Mehnert, JM | 4 |
| Malhotra, J | 1 |
| Cerchio, R | 1 |
| Marinaro, C | 1 |
| Foo, TK | 1 |
| Xia, B | 1 |
| Lee, JH | 2 |
| Dudek, L | 1 |
| Jeong, BS | 3 |
| Li, J | 2 |
| Schenkel, JM | 1 |
| Sadimin, E | 1 |
| Kane, M | 1 |
| Lin, H | 1 |
| Shih, WJ | 2 |
| Goydos, JS | 10 |
| Shah, R | 1 |
| Singh, SJ | 1 |
| Eddy, K | 1 |
| Filipp, FV | 1 |
| Wangari-Talbot, J | 2 |
| Shin, SS | 4 |
| Schiff, D | 2 |
| Sierra, J | 1 |
| Yu, LJ | 3 |
| Khan, A | 2 |
| Haffty, B | 2 |
| Wen, Y | 2 |
| Koo, J | 1 |
| Lin, Y | 1 |
| Cohen-Sola, KA | 1 |
| Yip, D | 1 |
| Le, MN | 2 |
| Chan, JL | 3 |
| Mehnert, JA | 1 |
| Yudd, A | 1 |
| Kempf, J | 1 |
| Rosenberg, SA | 1 |
| Nabatian, AS | 1 |
| Merrigan, KT | 1 |
| Cohen-Solal, KA | 2 |
| Khan, AJ | 1 |
| Wall, B | 1 |
| Ahlawat, S | 1 |
| Green, C | 1 |
| Haffty, BG | 1 |
| Lee, HJ | 2 |
| Rosenberg, S | 1 |
| Namkoong, J | 2 |
| Abushahba, W | 1 |
| Olabisi, OO | 1 |
| Boregowda, RK | 1 |
| Liu, F | 1 |
| Lasfar, A | 1 |
| Marín, YE | 1 |
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| A Phase I Study to Evaluate the Safety of Trigriluzole (FC-4157/BHV-4157) in Combination With PD-1 Blocking Antibodies[NCT03229278] | Phase 1 | 14 participants (Actual) | Interventional | 2017-10-03 | Completed | ||
| A Phase II Trial of Riluzole in Patients With Advanced Melanoma[NCT00866840] | Phase 2 | 13 participants (Actual) | Interventional | 2009-04-30 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||
The MTD of trigriluzole in combination with nivolumab will be identified. The MTD will then be tested in combination with pembrolizumab using the same escalate/de-escalate/stay rules. Data on the adverse event type, severity and frequency will be recorded. (NCT03229278)
Timeframe: Four weeks
| Intervention | mg (Number) |
|---|---|
| All Participants | 420 |
A DLT was any Grade 3 or 4 adverse event (AE) using the Common Terminology Criteria for Adverse Events Version 3.0 (CTCAE 3.0) that was possibly Trigriluzole or Nivolumab related. CTCAE 3.0 Grade 3 is a severe AE and Grade 4 is a life- threatening or disabling AE. DLTs were collected to determine the Maximum-Tolerated Dose (MTD), which is defined as the dose level below the dose at which 33% of participants experienced a DLT. (NCT03229278)
Timeframe: Four weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Experimental: Nivolumab 240mg IV Every 2 Weeks - Trigriluzole 140 mg Taken by Mouth Daily (PO) | 0 |
| Experimental: Nivolumab 240mg IV Every 2 Weeks - Trigriluzole 140 mg PO Twice a Day (BID) | 0 |
| Experimental: Nivolumab 240mg IV Every 2 Weeks - Trigriluzole 140 mg /280mg | 1 |
| Experimental: Nivolumab 240mg IV Every 2 Weeks - Trigriluzole 280mg PO BID | 2 |
Continuous variables will be presented by summary statistics (such as mean, median, standard error and 95% confidence intervals [CI]) and the categorical variables by frequency distributions (i.e., frequency counts, percentages and 95% CI). (NCT03229278)
Timeframe: Up to 3 years
| Intervention | percentage of participants (Number) |
|---|---|
| Nivolumab 240mg IV Every 2 Weeks - Trigriluzole 280mg PO BID | 7 |
1 review available for riluzole and Malignant Melanoma
| Article | Year |
|---|---|
The current management of brain metastasis in melanoma: a focus on riluzole.
Topics: Brain Neoplasms; Humans; Melanoma; Neuroprotective Agents; Riluzole | 2015 |
3 trials available for riluzole and Malignant Melanoma
| Article | Year |
|---|---|
A phase Ib dose-escalation study of troriluzole (BHV-4157), an oral glutamatergic signaling modulator, in combination with nivolumab in patients with advanced solid tumors.
Topics: Bayes Theorem; Carcinoma, Renal Cell; Enzyme Inhibitors; Glutamates; Humans; Kidney Neoplasms; Melan | 2022 |
A phase II trial of riluzole, an antagonist of metabotropic glutamate receptor 1 (GRM1) signaling, in patients with advanced melanoma.
Topics: Adult; Down-Regulation; Female; Humans; Male; MAP Kinase Signaling System; Melanoma; Middle Aged; Re | 2018 |
A phase 0 trial of riluzole in patients with resectable stage III and IV melanoma.
Topics: Blotting, Western; Caspase 3; Enzyme Activation; Excitatory Amino Acid Antagonists; Extracellular Si | 2009 |
11 other studies available for riluzole and Malignant Melanoma
| Article | Year |
|---|---|
Riluzole prodrugs for melanoma and ALS: design, synthesis, and in vitro metabolic profiling.
Topics: Amyotrophic Lateral Sclerosis; Animals; Cytochrome P-450 CYP1A2; Drug Design; Drug Stability; Humans | 2012 |
Nonhomologous end-joining repair is likely involved in the repair of double-stranded DNA breaks induced by riluzole in melanoma cells.
Topics: Cell Line, Tumor; DNA Breaks, Double-Stranded; DNA End-Joining Repair; DNA Repair; Humans; Melanoma; | 2020 |
Concurrent Targeting of Glutaminolysis and Metabotropic Glutamate Receptor 1 (GRM1) Reduces Glutamate Bioavailability in GRM1
Topics: Animals; Apoptosis; Benzeneacetamides; Biological Availability; Cell Proliferation; Drug Therapy, Co | 2019 |
Disruption of GRM1-mediated signalling using riluzole results in DNA damage in melanoma cells.
Topics: Acetylcysteine; Apoptosis; Biopsy; Cell Line, Tumor; DNA Breaks, Double-Stranded; DNA Damage; Gene K | 2014 |
Activation of the glutamate receptor GRM1 enhances angiogenic signaling to drive melanoma progression.
Topics: Angiogenesis Inhibitors; Animals; Cell Movement; Heterocyclic Compounds, 3-Ring; Humans; Hypoxia-Ind | 2014 |
Riluzole is a radio-sensitizing agent in an in vivo model of brain metastasis derived from GRM1 expressing human melanoma cells.
Topics: Animals; Brain Neoplasms; Cell Line, Tumor; Clone Cells; Disease Models, Animal; Humans; Luciferases | 2015 |
The glutamate release inhibitor Riluzole decreases migration, invasion, and proliferation of melanoma cells.
Topics: Cell Division; Cell Line, Tumor; Cell Movement; Excitatory Amino Acid Antagonists; Extracellular Sig | 2010 |
Riluzole enhances ionizing radiation-induced cytotoxicity in human melanoma cells that ectopically express metabotropic glutamate receptor 1 in vitro and in vivo.
Topics: Animals; Apoptosis; Brain Neoplasms; Caspase 3; Cell Cycle; Cell Line, Tumor; Cell Survival; Combine | 2011 |
Glutamatergic pathway targeting in melanoma: single-agent and combinatorial therapies.
Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Benzenesulfonates; Cell Cycle; Cell Line, T | 2011 |
Non-canonical Smads phosphorylation induced by the glutamate release inhibitor, riluzole, through GSK3 activation in melanoma.
Topics: Animals; Cell Line, Tumor; Gene Expression Regulation, Neoplastic; Glutamic Acid; Glycogen Synthase | 2012 |
Metabotropic glutamate receptor 1 and glutamate signaling in human melanoma.
Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Proliferation; Drug Evaluation, Preclinical; Glutami | 2007 |