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Content Update

September 9, 2021

Amivantamab Approved for Treatment of EGFR exon 20 insertion-mutated Locally Advanced or Metastatic Non-small Cell Lung Cancer: Amivantamab is a bispecific EGFR receptor and MET receptor-directed antibody approved as a single agent for the treatment of EGFR exon 20 insertion-mutated locally advanced or metastatic non-small cell lung cancer in patients who have progressed on or after platinum based therapy. Amivantamab binds to both EGFR and MET, blocking ligand binding and which disrupts signaling pathways and causes degradation of EGFR and MET. In a phase 1 single arm trial enrolling 81 patients with EGFR exon 20 insertion mutations, the overall response rate was 40% with a median progression free survival of 8.3 months. Common adverse events included rash, infusion reactions, and hypokalemia.

Content Update

June 14, 2021

Sotorasib Approved for Treatment KRAS G12C-mutated Locally Advanced or Metastatic Non-small Cell Lung Cancer: Sotorasib is a RAS inhibitor approved as a single agent for treatment of RAS G12C-mutated locally advanced or metastatic non-small cell lung cancer in patients who have received at least one prior therapy. Sotorasib is small molecule that covalently and irreversibly binds to the unique cysteine of KRAS G12C, which locks the protein in an inactive state that prevents further RAS signaling, ultimately inhibiting cell growth and promoting apoptosis. In a phase 2 single arm trial enrolling 124 patients with KRAS G12C mutations, the overall response rate was 37% with a median progression free survival of 6.8 months. Common adverse events included diarrhea, myopathy, and hepatotoxicity.

Content Update

May 28, 2020

Selpercatinib Approved for Treatment of RET Fusion-Positive Non-small-cell Lung Cancer (NSCLC) And Thyroid Cancer: Selpercatinib (Retevmo) is indicated for adults with RET fusion-positive NSCLC and adults and children older than age 12 with RET fusion-positive thyroid cancer. A trial involving 144 patients with NSCLC and 143 patients with thyroid cancer who had advanced or metastatic RET fusion-positive disease gave patients selpercatinib 160 mg orally twice a day. The overall response rate was 64% (95% CI: 54%, 73%) in NSCLC patients who received prior therapy, 69% (95% CI: 55%, 81%) in treatment-naïve individuals, and 73% (95% CI: 62%, 82%) in treatment-naïve patients with thyroid cancer. Common adverse effects were diarrhea and hypertension.

Content Update

March 7, 2020

Tazemetostat Approved for Treatment of Sarcoma: Tazemetostat (Tazverik) is the first EZH2 inhibitor approved by the FDA and is indicated for adults and children older than 16 for the treatment of epithelioid sarcoma. In a phase II, open-label trial of patients with locally-advanced or metastatic epithelioid sarcoma, 62 patients were treated with tazemetostat 800 mg orally twice a day. The disease control rate (defined as complete responses, partial response and stable disease) was 26% (15/62) with a median overall survival of 82.4 weeks (95% CI: 47.4, not estimable) for all 62 pts. ...

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