Therapy Detail
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| Therapy Name | Binimetinib + PF-07799933 |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Binimetinib | Mektovi | ARRY-162|ARRY-438162|MEK162 | MEK inhibitor (Pan) 26 MEK1 Inhibitor 26 MEK2 Inhibitor 24 | Mektovi (binimetinib) inhibits MEK1 and MEK2 resulting in inhibition of growth factor-mediated signaling and decreased tumor cell proliferation (PMID: 23587417). Mektovi (binimetinib) in combination with Braftovi (encorafenib) is FDA approved for use in patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation (FDA.gov). |
| PF-07799933 | PF07799933|PF 07799933|ARRY440|ARRY 440|ARRY-440 | BRAF Inhibitor 25 | PF-07799933 inhibits BRAF mutations, including class 1, 2, and 3 mutations, which potentially leads to decreased downstream Erk signaling and inhibition of tumor growth (PMID: 38691346). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BRAF del exon2-8 BRAF V600E | papillary thyroid carcinoma | predicted - sensitive | Binimetinib + PF-07799933 | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with the combination of PF-07799933 and Mektovi (binimetinib) resulted in a partial response with a tumor reduction of 80% in a patient with papillary thyroid carcinoma harboring BRAF V600E and a deletion of BRAF exons 2-8 (reported as p48 splice variant) (PMID: 38691346; NCT05355701). | 38691346 |
| BRAF del exon4-8 BRAF V600E | melanoma | sensitive | Binimetinib + PF-07799933 | Preclinical - Pdx | Actionable | In a preclinical study, treatment with the combination of PF-07799933 and Mektovi (binimetinib) resulted in tumor regression in a patient-derived xenograft (PDX) model of melanoma harboring BRAF V600E and a BRAF exon 4-8 deletion variant (reported as p61 splice variant) (PMID: 38691346). | 38691346 |
| BRAF V600E | high grade glioma | predicted - sensitive | Binimetinib + PF-07799933 | Case Reports/Case Series | Actionable | In a Phase I trial, the addition of Mektovi (binimetinib) to treatment with PF-07799933 resulted in a partial response in a patient with high grade glioma harboring BRAF V600E (PMID: 38691346; NCT05355701). | 38691346 |
| BRAF V600E | melanoma | predicted - sensitive | Binimetinib + PF-07799933 | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with the combination of PF-07799933 and Mektovi (binimetinib) resulted in a partial response in 2 patients with melanoma harboring BRAF V600E and stable disease in 1 patient (PMID: 38691346; NCT05355701). | 38691346 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT05355701 | Phase I | Binimetinib + PF-07799933 PF-07799933 Cetuximab + PF-07799933 | A Study to Learn About the Study Medicine Called PF-07799933 in People With Advanced Solid Tumors With BRAF Alterations. | Recruiting | USA | ISR | CAN | 0 |
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