Dear Colleagues,

Endocrine agents, for the treatment of hormone receptor positive breast cancer patients, include selective estrogen receptor modulators (SERMs), aromatase inhibitors (AIs), and selective estrogen receptor downregulators (SERDs). The first generation SERM, tamoxifen, has been used for over four decades in the standard of care of estrogen receptor positive (ER+)  breast cancer in both pre- and postmenopausal patients. Second and third generation SERMs, such as raloxifene, lasofoxifen, and bazedoxifen, have been developed as more potent and selective ER antagonists, and are used for osteoporosis and breast cancer prevention, but have not been approved for hormone therapy for breast cancer patients. Major clinical challenges with SERM therapy include de novo and acquired resistance, which inevitably lead to recurrence of disease and mortality. Fulvetrant is currently the only SERD that has been approved for clinical use, and it has a low bioavailability and can only be administered as an intramuscular injection depot. There is clearly an urgent need to improve breast cancer patient survival and quality of life by developing next generation SERM/SERD hybrids and more efficacious SERDs that are not cross-resistant to tamoxifen and AI treatment. The present Special Issue is aimed at covering new developments in the design, synthesis, and biological evaluation of novel SERMs, SERDs, and SERM/SERD hybrids that may hold clinical potential as breast cancer treatment agents. 

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

• SERM
• SERD
• ER+ breast cancer
• endocrine therapy
• endocrine resistance
• ER downregulation
• hot flash
• osteoporosis
• antiestrogen