exemestane

P=N/A, N=329, Completed, Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins | Active, not recruiting --> Completed

P2, N=200, Recruiting, Oana Danciu | Trial completion date: Dec 2027 --> Aug 2029 | Trial primary completion date: Dec 2024 --> Aug 2028

Compounds 1-6 showed a significant aromatase inhibition with IC50 values in the range of 2.01-3.13 μM as compared to the standard drug, exemestane (IC50 = 0.21 ± 0.16 μM)...Moreover, compounds 1-6 were found as non-cytotoxic to BJ (Human fibroblast) normal cell line. Hence, these molecules can be further studied for optimization as potential aromatase inhibitors against breast cancer.

P3, N=460, Recruiting, Jiangsu Simcere Pharmaceutical Co., Ltd. | Initiation date: Feb 2025 --> Nov 2024

Hormonal or endocrine therapy includes selective estrogen receptor modulators (SERMs) such as raloxifene, tamoxifen and toremifene, selective estrogen-receptor degraders (SERDs) including elacestrant and fulvestrant, and aromatase inhibitors such as anastrozole, letrozole, and exemestane...These agents include taxanes (docetaxel, nab-paclitaxel, and paclitaxel), anthracyclines (doxorubicin, epirubicin), anti-metabolites (capecitabine, gemcitabine, fluorouracil, methotrexate), alkylating agents (carboplatin, cisplatin, and cyclophosphamide), and drugs that target microtubules (eribulin, ixabepilone, ado-trastuzumab emtansine). Patients with ER-positive tumors are treated with 5-10 years of endocrine therapy and chemotherapy. For patients with metastatic breast cancer, standard first-line and follow-up therapy options include targeted approaches such as CDK4/6 inhibitors, PI3K inhibitors, PARP inhibitors, and anti-PDL1 immunotherapy, depending on the tumor type and molecular profile.

P1, N=72, Active, not recruiting, Eisai Co., Ltd. | Trial completion date: Dec 2024 --> Mar 2026 | Trial primary completion date: Dec 2024 --> Mar 2026

P3, N=460, Recruiting, Jiangsu Simcere Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting

P3, N=3832, Not yet recruiting, Region Örebro County | Initiation date: May 2024 --> Jan 2025

Introduction The INGE-B trial (NCT02894398) aimed to confirm the efficacy and safety data from the PALOMA trials for patients treated first line (1L) with palbociclib (PAL) and letrozole or 1L and later line with PAL and fulvestrant. Conclusion The INGE-B trial demonstrated good efficacy and tolerability of PAL with letrozole (1L) or fulvestrant (first and later line) in accordance with the PALOMA-trials. In addition, the so far lacking proof of efficacy and safety of PAL in combination with anastrozole or exemestane in 1L and with letrozole in later line was provided by INGE-B.

Endocrine therapy plus CDK 4/6i represents an effective treatment, regardless of HER2 status (low/zero). Second-line agents did not differ significantly in terms of TTD. Endocrine resistant cancers exhibit poor response to CDK 4/6i.

P3, N=460, Not yet recruiting, Jiangsu Simcere Pharmaceutical Co., Ltd.

P2, N=90, Active, not recruiting, Dana-Farber Cancer Institute | Recruiting --> Active, not recruiting | Trial primary completion date: Jan 2026 --> Jun 2025

P3, N=1156, Not yet recruiting, Alliance for Clinical Trials in Oncology

Part 1 included treatment with fulvestrant (FUL) 500 mg + E7090 (105 or 140 mg) or exemestane (EXE) 25 mg + E7090 (105 or 140 mg). These results emphasize that FGFR pathway activation evaluated with mRNA expression of selected genes at BL—rather than FGFR gene abnormalities—is a key molecular determinant for sensitivity to E7090, an FGFR inhibitor. Future validation of these biomarkers is necessary in a larger population of people with ER+/HER2− BC.

MAINTAIN was the first randomized controlled trial to demonstrate a significant progression-free survival (PFS) benefit for HR+, HER2- MBC patients who switched ET (fulvestrant or exemestane) and received the CDK4/6i ribociclib compared to ET plus placebo after progressing on prior CDK4/6i and ET. In the phase II MAINTAIN trial, sTKa was a predictive biomarker for response to switching ET + continuing CDK4/6i in HR+, HER2- MBC pts following progression on CDK4/6i and ET. Low (<250 DuA) C2D1 sTKa levels predicted a positive treatment response, especially among those receiving ribociclib+ET. sTKa dynamics from baseline to C2D1 were prognostic, providing insights into PFS outcomes.

Therapies targeting mutations in this pathway approved in conjunction with endocrine therapy include alpelisib, everolimus and capivasertib...She received nab-paclitaxel/atezolizumab for 4 months, letrozole and abemaciclib for 2 months, letrozole alone for 6 months, and letrozole and ribociclib for 6 weeks. Given presence of PIK3CA mutation, 4th line treatment with fulvestrant and alpelisib was planned...After progressing on capecitabine after 2 months, alpelisib with exemestane was initiated...Due to a low ejection fraction despite work with cardiooncology, she was not a candidate for trastuzumab deruxtecan. She progressed on oral cyclophosphamide and methotrexate after 2 months and Sacituzumab govitecan after 3 months...Comprehensive biomarker assessment is needed to identify patients who may benefit from sequential therapies. There is a need for trials comparing therapies that target the PI3K pathway at distinct points, potential sequencing of these therapies, and the optimal sequence strategy.

P2, N=120, Recruiting, Merck Sharp & Dohme LLC | Not yet recruiting --> Recruiting

P2, N=200, Recruiting, Oana Danciu | Active, not recruiting --> Recruiting

P3, N=4220, Recruiting, Stemline Therapeutics, Inc. | Not yet recruiting --> Recruiting

P1/2, N=138, Completed, Hoffmann-La Roche | Active, not recruiting --> Completed

P3, N=320, Active, not recruiting, Genentech, Inc. | Recruiting --> Active, not recruiting | Trial primary completion date: Oct 2024 --> Mar 2026

P=N/A, N=1900, Recruiting, Pfizer | Trial completion date: Apr 2028 --> Mar 2029

P3, N=500, Recruiting, AstraZeneca | Trial completion date: Jul 2030 --> Oct 2030

P2; Sunitinib plus exemestane was associated with substantial yet reversible toxicities, providing safety, efficacy and biological impact insights of combining an antiangiogenic drug with hormone therapy in early-stage breast cancer.Trial registration: Registered with ClinicalTrials.gov, NCT00931450. 02/07/2009.

P2, N=120, Not yet recruiting, Merck Sharp & Dohme LLC | Trial primary completion date: Jan 2027 --> May 2027

P2, N=38, Not yet recruiting, OHSU Knight Cancer Institute

P2, N=620, Recruiting, Fudan University | N=140 --> 620

P3; Active, not recruiting --> Completed

P3, N=504, Not yet recruiting, Danish Breast Cancer Cooperative Group | Phase classification: P4 --> P3 | N=250 --> 504

P4, N=130, Completed, German Breast Group | Recruiting --> Completed | Trial completion date: Mar 2023 --> Aug 2024 | Trial primary completion date: Mar 2023 --> Aug 2024

P2, N=200, Active, not recruiting, Oana Danciu | Recruiting --> Active, not recruiting

From molecular docking and analysis of interactions with the amino acid residues of the binding cavity, it was found that the amino acid residues interacting with the non-steroidal inhibitors exhibited π-stacking interactions with PHE134, PHE 221, and TRP 224, while the steroidal drug exemestane lacked π-stacking interactions...Additionally, anthraquinone compounds with minor structural modification can also serve to be potential aromatase inhibitors. The in silico protocol utilised can be useful in the drug discovery process for development of new leads from structurally diverse set of natural products that are comparable to the drugs used clinically in breast cancer therapy.

P2, N=60, Suspended, University of Washington | Recruiting --> Suspended

P4, N=250, Not yet recruiting, Danish Breast Cancer Cooperative Group

There are two main patterns of P16 and P53 expression, P16-positive/P53 wild-type and P16-negative/P53-mutant, but no positive expression of both has been seen so far. It is worth noting that we reported the second case of PESCC with a history of breast cancer, where the patient had been taking the oral aromatase inhibitor drug (exemestane) for a long period of time to reduce the estrogen level, indicating the low estrogen level may be also a key factor in the pathogenesis of PESCC.

P1/2, N=138, Active, not recruiting, Hoffmann-La Roche | Trial completion date: Dec 2024 --> Sep 2024

P2, N=37, Active, not recruiting, Medical College of Wisconsin | Trial completion date: Jul 2024 --> Mar 2025

P1, N=193, Active, not recruiting, Eli Lilly and Company | Recruiting --> Active, not recruiting | N=400 --> 193

P1/2, N=138, Active, not recruiting, Hoffmann-La Roche | Trial primary completion date: Dec 2024 --> Sep 2024

P2, N=247, Completed, Pfizer | Active, not recruiting --> Completed

P3, N=500, Recruiting, AstraZeneca | Not yet recruiting --> Recruiting | Initiation date: Apr 2024 --> Aug 2024

P2, N=83, Active, not recruiting, Shayna Showalter, MD | Trial primary completion date: Mar 2024 --> Jun 2024