Overview
Exemestane is an oral steroidal aromatase inhibitor used in the adjuvant treatment of hormonally-responsive (also called hormone-receptor-positive, estrogen-responsive) breast cancer in postmenopausal women. It irreversibly binds to the active site of the enzyme resulting in permanent inhibition.
Background
Exemestane is an oral steroidal aromatase inhibitor used in the adjuvant treatment of hormonally-responsive (also called hormone-receptor-positive, estrogen-responsive) breast cancer in postmenopausal women. It irreversibly binds to the active site of the enzyme resulting in permanent inhibition.
Indication
For the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy.
Associated Conditions
- Stage I Breast Cancer
- Refractory, advanced Breast cancer
Research Report
An Analytical Report on Two Paradigms in Oncologic Therapy: The Established Aromatase Inhibitor Exemestane and the Investigational Treg Modulator GIM-531
Part I: Exemestane (Aromasin®) - A Comprehensive Clinical and Pharmacological Profile
This section provides a definitive review of Exemestane, leveraging its extensive history of clinical use and regulatory documentation to build a complete profile of a mature, yet still critical, oncologic agent.
1.1. Molecular Identity and Physicochemical Properties
Exemestane is a cornerstone therapeutic agent in the management of hormone receptor-positive breast cancer. Its efficacy is intrinsically linked to its unique chemical structure and physical properties, which dictate its biological activity and clinical application.
Chemical Structure and Classification
Exemestane is an oral steroidal aromatase inhibitor.[1] Its chemical designation is 6-methylenandrosta-1,4-diene-3,17-dione.[1] As a steroidal compound, it is structurally analogous to the natural substrate of the aromatase enzyme, androstenedione.[2] This structural mimicry is not a coincidence but rather the fundamental basis of its mechanism of action, allowing it to be recognized and processed by the target enzyme, which ultimately leads to the enzyme's inactivation. It is classified as a 17-oxo steroid and a 3-oxo-Delta(1),Delta(4)-steroid, deriving from a hydride of an androstane.[1]
Molecular Formula and Weight
The molecular formula of exemestane is C20H24O2, corresponding to a molecular weight of 296.41 g/mol [3] and an average weight of 296.4034 g/mol.[2] Its monoisotopic mass is 296.177630004 Da.[1]
Physical Characteristics
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
---|---|---|---|---|---|
2025/06/17 | Phase 3 | Not yet recruiting | Shandong Suncadia Medicine Co., Ltd. | ||
2025/05/20 | Phase 2 | Not yet recruiting | |||
2025/05/04 | Phase 2 | Active, not recruiting | CSPC ZhongQi Pharmaceutical Technology Co., Ltd. | ||
2024/11/08 | Phase 3 | Recruiting | |||
2024/11/04 | Phase 3 | Recruiting | |||
2024/10/08 | Phase 2 | Recruiting | |||
2025/03/11 | Phase 3 | Recruiting | |||
2024/05/24 | Phase 2 | Recruiting | |||
2024/04/24 | Phase 3 | Recruiting | |||
2024/04/15 | Phase 2 | Not yet recruiting | Andrea DeCensi |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
---|---|---|---|---|---|
Physicians Total Care, Inc. | 54868-5261 | ORAL | 25 mg in 1 1 | 1/4/2010 | |
Bryant Ranch Prepack | 63629-2056 | ORAL | 25 mg in 1 1 | 12/30/2021 | |
Amneal Pharmaceuticals LLC | 65162-240 | ORAL | 25 mg in 1 1 | 11/19/2022 | |
Florida Pharmaceutical Products, LLC | 71921-190 | ORAL | 25 mg in 1 1 | 6/19/2023 | |
Breckenridge Pharmaceutical, Inc. | 51991-005 | ORAL | 25 mg in 1 1 | 1/25/2024 | |
A-S Medication Solutions | 50090-5193 | ORAL | 25 mg in 1 1 | 5/1/2018 | |
Upsher-Smith Laboratories, Inc. | 0832-0595 | ORAL | 25 mg in 1 1 | 1/31/2022 | |
Pharmacia & Upjohn Company LLC | 0009-7663 | ORAL | 25 mg in 1 1 | 11/1/2021 | |
Eirgen Pharma Ltd | 44278-025 | ORAL | 25 mg in 1 1 | 2/9/2021 | |
Greenstone LLC | 59762-2858 | ORAL | 25 mg in 1 1 | 11/1/2021 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
---|---|---|---|
No EMA approvals found for this drug. |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
AROMASIN TABLET 25mg | SIN11398P | TABLET, SUGAR COATED | 25 mg | 9/20/2000 | |
EXACCORD 25 FILM COATED TABLET 25 MG | SIN16062P | TABLET, FILM COATED | 25 mg | 12/18/2020 | |
EXEMESTANE ALVOGEN FILM COATED TABLETS 25MG | SIN14499P | TABLET, FILM COATED | 25.00 mg | 1/27/2014 | |
EXEDRAL 25 FILM-COATED TABLET 25MG | SIN16646P | TABLET, FILM COATED | 25.0mg | 11/22/2022 | |
AROMASTAN F.C. TABLET 25MG | SIN15232P | TABLET, FILM COATED | 25 mg | 5/11/2017 | |
EXEMESTANE STADA FILM COATED TABLET 25mg | SIN14757P | TABLET, FILM COATED | 25mg | 3/20/2015 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
---|---|---|---|---|---|
Exemestane Capsules | 国药准字H20020006 | 化学药品 | 胶囊剂 | 6/5/2024 | |
Exemestane Capsules | 国药准字H20020011 | 化学药品 | 胶囊剂 | 4/24/2020 | |
Exemestane Tablets | m/s cipla ltd. | 国药准字HJ20240026 | 化学药品 | 片剂 | 5/21/2024 |
Exemestane Tablets | 国药准字H20253283 | 化学药品 | 片剂 | 1/24/2025 | |
Exemestane Tablets | 国药准字H20020008 | 化学药品 | 片剂 | 3/29/2021 | |
Exemestane Tablets | 国药准字H20244096 | 化学药品 | 片剂 | 6/18/2024 | |
Exemestane Tablets | 国药准字HJ20160054 | 化学药品 | 片剂 | 9/4/2020 | |
Exemestane Tablets | 国药准字HJ20160053 | 化学药品 | 片剂 | 9/4/2020 | |
Exemestane Tablets | 国药准字H20020004 | 化学药品 | 片剂 | 3/31/2020 | |
Exemestane Tablets | 国药准字HJ20160052 | 化学药品 | 片剂 | 9/4/2020 |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
---|---|---|---|---|---|
EXEMESTANE ALVOGEN FILM-COATED TABLETS 25MG | N/A | N/A | N/A | 8/7/2012 |
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
---|---|---|---|---|---|
EXEMEST exemestane 25mg tablet blister pack | 281352 | Medicine | A | 2/9/2017 | |
EXEMESTANE SANDOZ | 174337 | Medicine | A | 9/12/2011 | |
APO-EXEMESTANE | 177312 | Medicine | A | 10/6/2011 | |
EXEMESTANE SCP exemestane 25 mg tablet blister pack | 177310 | Medicine | A | 10/6/2011 | |
AROMASIN exemestane 25mg tablet blister pack | 76369 | Medicine | A | 11/30/2000 | |
EXEMESTANE INTAS exemestane 25mg tablet blister pack | 281350 | Medicine | A | 2/9/2017 | |
EXEMESTANE GH exemestane 25mg tablet blister pack | 167858 | Medicine | A | 4/4/2011 | |
EXEMESTANE-WGR exemestane 25 mg tablet blister pack | 177313 | Medicine | A | 10/6/2011 |