Braftovi (encorafenib)

Trastuzumab-based combinations and HER2-selective tyrosine kinase inhibitors such as tucatinib have demonstrated durable responses and favorable safety profiles in heavily pretreated patients. This review summarizes current evidence from pivotal phase II and III clinical trials, translational studies, and real-world data evaluating EGFR-, BRAF-, and HER2-directed therapies in colorectal cancer. Particular emphasis is placed on biomarker-guided patient selection, mechanisms of resistance, and emerging combination strategies that continue to refine precision oncology approaches in mCRC.

In a compound screen on melanoma cells, we identified FX-11 as one of the compounds inhibiting the growth of sensitive and Encorafenib/Binimetinib-resistant 624Mel and Wm3248 melanoma cells. Taken together, we provide evidence that FX-11 inhibits the growth of melanoma cells, including drug-resistant ones, through an AMPK-dependent mechanism by acting as a mitochondrial uncoupler. Our data do not support that FX-11 acts as an LDH inhibitor.

Combination therapy of encorafenib plus binimetinib for unresectable BRAF V600-mutated thyroid cancer was associated with generally maintained HR-QoL. Considering the efficacy and safety data from the trial, the regimen may provide clinical benefits while maintaining HR-QoL.

P1/2, N=101, Completed, Erasca, Inc. | Active, not recruiting --> Completed

P2, N=25, Recruiting, Vall d'Hebron Institute of Oncology | Not yet recruiting --> Recruiting

P2, N=10, Active, not recruiting, UNICANCER | Trial completion date: Apr 2029 --> Mar 2026 | Trial primary completion date: Apr 2025 --> Mar 2026

P2, N=84, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Feb 2026 --> Sep 2026 | Trial primary completion date: Feb 2026 --> Sep 2026

This model successfully described the PK of encorafenib over time and across tumor types. No dose modifications are suggested on the basis of intrinsic or extrinsic factors evaluated.

P2, N=38, Terminated, Pfizer | Active, not recruiting --> Terminated; Study terminated due to inability to recruit the target number of patients. There were no safety and/or efficacy concerns involved in the decision to stop enrollment.

These findings demonstrate that clinically meaningful survival gains may not translate into economic value in first-line settings. This study underscores the importance of incorporating economic evidence into early treatment adoption decisions and highlights the need for pricing approaches that better align costs with patient benefit.

She was initially treated with Vemurafenib and Cobimetinib, achieving complete remission. However, due to cumulative toxicities, therapy was switched to Encorafenib and Binimetinib in February 2023...Management included Binimetinib dose reduction and topical ketorolac, resulting in initial improvement, although the CME recurred several months later...The patient ultimately began immunotherapy with Nivolumab and Ipilimumab, but died in February 2024 due to refractory abdominal septic shock. This case highlights the importance of early ophthalmologic monitoring and interdisciplinary collaboration in patients receiving MEK inhibitors.