First Approval of Elacestrant as a Selective Estrogen Receptor Degrader for the Treatment of Metastatic Breast Cancer-Reference-Cited by-同舟云学术

First Approval of Elacestrant as a Selective Estrogen Receptor Degrader for the Treatment of Metastatic Breast Cancer

Published:2024-02 Issue:7 Volume:31 Page:791-795
ISSN:0929-8673
Container-title:Current Medicinal Chemistry
language:en
Short-container-title:CMC

Author:

De Surya K.¹²

Affiliation:

1. Department of Chemistry, Conju-Probe, San Diego, California, USA

2. Bharath University, Chennai, Tamil Nadu, 600126, India

Abstract

Abstract: Elacestrant was approved by the US FDA on January 27, 2023, for treating postmenopausal women or adult men with estrogen receptor (ER)-positive, HER2- negative, ESR1-mutated advanced or metastatic breast cancer with disease progression prior to using at least one line of endocrine therapy. In this short perspective, physicochemical properties, dosage and administration, mechanism of action, pharmacodynamics, pharmacokinetics, drug interaction, and treatment-related adverse reactions of elacestrant are summarized.

Publisher

Bentham Science Publishers Ltd.

Subject

Pharmacology,Molecular Medicine,Drug Discovery,Biochemistry,Organic Chemistry

Reference17 articles.

1. Bidard F.C.; Kaklamani V.G.; Neven P.; Streich G.; Montero A.J.; Forget F.; Mouret-Reynier M.A.; Sohn J.H.; Taylor D.; Harnden K.K.; Khong H.; Kocsis J.; Dalenc F.; Dillon P.M.; Babu S.; Waters S.; Deleu I.; García Sáenz J.A.; Bria E.; Cazzaniga M.; Lu J.; Aftimos P.; Cortés J.; Liu S.; Tonini G.; Laurent D.; Habboubi N.; Conlan M.G.; Bardia A.; Elacestrant (oral selective estrogen receptor degrader) versus standard endocrine therapy for estrogen receptor–positive, human epidermal growth factor receptor 2–negative advanced breast cancer: Results from the randomized phase III EMERALD trial. J Clin Oncol 2022,40(28),3246-3256

2. Wang Y.; Tang S.C.; The race to develop oral SERDs and other novel estrogen receptor inhibitors: Recent clinical trial results and impact on treatment options. Cancer Metastasis Rev 2022,41(4),975-990

3. Lloyd M.R.; Wander S.A.; Hamilton E.; Razavi P.; Bardia A.; Next-generation selective estrogen receptor degraders and other novel endocrine therapies for management of metastatic hormone receptor-positive breast cancer: Current and emerging role. Ther Adv Med Oncol 2022,14

4. Bardia A.; Kaklamani V.; Wilks S.; Weise A.; Richards D.; Harb W.; Osborne C.; Wesolowski R.; Karuturi M.; Conkling P.; Bagley R.G.; Wang Y.; Conlan M.G.; Kabos P.; Phase I.; Phase I study of elacestrant (RAD1901), a novel selective estrogen receptor degrader, in ER-Positive, HER2-negative advanced breast cancer. J Clin Oncol 2021,39(12),1360-1370

5. Bihani T.; Patel H.K.; Arlt H.; Tao N.; Jiang H.; Brown J.L.; Purandare D.M.; Hattersley G.; Garner F.; Elacestrant (RAD1901), a Selective Estrogen Receptor Degrader (SERD), has antitumor activity in multiple ER+ breast cancer patient-derived xenograft models. Clin Cancer Res 2017,23(16),4793-4804