Letrozole

Generic Name
Letrozole
Brand Names
Femara, Kisqali Femara Co-pack
Drug Type
Small Molecule
Chemical Formula
C17H11N5
CAS Number
112809-51-5
Unique Ingredient Identifier
7LKK855W8I
Background

Letrozole, or CGS 20267, is an oral non-steroidal type II aromatase inhibitor first described in the literature in 1990. It is a third generation aromatase inhibitor like exemestane and anastrozole, meaning it does not significantly affect cortisol, aldosterone, and thyroxine.

Letrozole was granted FDA approval on 25 July 1997.

Indication

Letrozole is indicated to treat postmenopausal women with hormone receptor (HR) positive early breast cancer, postmenopausal women with early breast cancer who have periviously been treated with tamoxifen, and postmenopausal women with HR+ or unknown advanced breast cancer. Letrozole, given with ribociclib, is indicated to treat pre, peri, and postmenopausal...

Associated Conditions
Advanced Breast Cancer, Anovulatory cycle, Epithelial Ovarian Cancer, HR+, HER2-, Advanced Breast Cancer, Stage I Breast Cancer, Metastatic HR + HER2 - breast cancer
Associated Therapies
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targetedonc.com
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The Targeted Pulse: Explore Highlighted Updates From This Year's SABCS on Breast

Palbociclib + standard therapy improved progression-free survival in hormone receptor–positive, HER2-positive metastatic breast cancer. No significant overall survival benefit observed among CDK4/6 inhibitor combinations in hormone receptor-positive/HER2-negative breast cancer. Patritumab deruxtecan showed similar efficacy to multiagent chemotherapy in high-risk hormone receptor-positive, HER2-negative breast cancer. Ciltacabtagene autoleucel achieved 100% complete response in high-risk smoldering multiple myeloma. Selinexor + ruxolitinib showed efficacy in myelofibrosis patients previously treated with ruxolitinib.
curetoday.com
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HER3-DXd With or Without Femara Effective for Some With High-Risk Breast Cancer

Patritumab deruxtecan with or without Femara showed similar treatment responses to multiagent chemotherapy in high-risk HR-positive, HER2-negative breast cancer, with fewer severe side effects. The phase 2 SOLTI VALENTINE trial reported pCR rates of 4% and ORR of 70% for ADC alone, 2.1% and 81.3% with Femara, and 4.2% and 70.8% for chemotherapy. The ADC also demonstrated antitumor activity and improved tolerability.
cancernetwork.com
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Early Breast Cancer Treatment Post the CDK4/6 Inhibitor Ribociclib's FDA Approval

Experts discussed the NATALEE trial and adjuvant ribociclib in breast cancer at an FDA Special Session, emphasizing the need for further studies on dosing and benefits. The trial included 5,101 patients, with 43% completing three years of adjuvant Kisqali. The FDA approved Kisqali in 2024 for HR-positive, HER2-negative early breast cancer, with postmarketing commitments for diversity and overall survival analyses.
curetoday.com
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Looking Ahead After Kisqali's FDA Approval for Adjuvant Treatment of Early Breast Cancer

Kisqali, a CDK4/6 inhibitor, shows promise in treating HR-positive, HER2-negative early breast cancer, as demonstrated by the NATALEE trial. The trial involved 5,101 patients, with Kisqali given for three years alongside an aromatase inhibitor. Despite its FDA approval in 2024, follow-up studies are ongoing to assess additional benefits, dosing strategies, and overall survival. The trial highlighted the need for more diverse patient representation and ongoing research into optimal treatment durations and doses.
formularywatch.com
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Optum Rx Switches Up Humira Biosimilar Coverage for 2025

Optum Rx prefers Amgen’s Amjevita over Sandoz’s Hyrimoz and Cyltezo on its 2025 commercial formularies, aiming to reduce costs and improve affordability. Humira remains on the formulary but with stricter controls. Biosimilars, including Humira’s, have struggled with adoption despite cost savings potential. Optum Rx also adds and removes various oncology and CNS medications for 2025.

Switches Up Humira Biosimilar Coverage for 2025

Optum Rx prefers Amgen’s Amjevita over Sandoz’s Hyrimoz and Cyltezo on its 2025 commercial formularies, aiming to reduce costs and improve affordability. Humira remains on the formulary but is subject to prior authorization. Biosimilars have struggled with low adoption despite cost advantages, but large PBMs like CVS Health are shifting towards biosimilars. Optum Rx also adds and removes various oncology and CNS medications from its 2025 formulary.
curetoday.com
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FDA Approves Kisqali Regimen for HR+/HER2- Early Breast Cancer

The FDA approved Kisqali with an aromatase inhibitor for postsurgical treatment of HR-positive, HER2-negative early breast cancer at high risk of recurrence. The efficacy was demonstrated in the phase 3 NATALEE trial, showing improved invasive disease-free survival. Side effects included neutropenia, liver-related issues, QT interval prolongation, and interstitial lung disease/pneumonitis.
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