Idoxifene
Idoxifene: An Investigated SERM
Idoxifene (also known by its International Nonproprietary Name (INN), US Adopted Name (USAN), and British Approved Name (BAN)), and previously identified under developmental code names CB-7432 and SB-223030, belongs to the category of nonsteroidal Selective Estrogen Receptor Modulators (SERM). It is structurally related to the triphenylethylene group and is alternatively termed pyrrolidino-4-iodotamoxifen. While it was being considered for clinical use, especially in the treatment of breast cancer and postmenopausal osteoporosis, it never progressed to commercialization.
Chemical and Pharmacological Background
- Structural Classification: Idoxifene is structurally a member of the triphenylethylene group, which associates it with other well-known SERMs. Its chemical structure is analogous to tamoxifen, with a pyrrolidino-4-iodo substitution.
- Mode of Action: As a SERM, Idoxifene modulates the estrogen receptor's activity, functioning either as an agonist or antagonist based on the target tissue[1].
Clinical Development
Idoxifene underwent extensive clinical trials to evaluate its therapeutic potential in two primary medical conditions:
- Breast Cancer: Idoxifene reached phase II clinical trials for its efficacy in treating breast cancer. Breast cancer cells often exhibit an over-expression of estrogen receptors, and modulating these receptors can offer therapeutic benefits[2].
- Postmenopausal Osteoporosis: Recognizing the influence of estrogen on bone mineral density, Idoxifene was explored in phase III clinical trials for its potential in treating osteoporosis in postmenopausal women[3].
Unfortunately, Idoxifene's development was halted in 1999, as it failed to demonstrate sufficient therapeutic efficacy in both of these conditions.
Challenges in Development
While the precise reasons for the discontinuation of Idoxifene's development aren't publicized in full detail, the generic challenges faced in the development of SERMs include:
- Efficacy: Achieving a balance where a SERM can suppress estrogenic activity in one tissue (like the breast) while promoting it in another (like bone) is intricate.
- Safety: All SERMs carry potential side effects, some of which may not be apparent until advanced stages of clinical trials.
Conclusion
Idoxifene, despite its initial promise as a potent SERM, did not meet the desired endpoints in clinical trials, reinforcing the inherent challenges in developing efficacious and safe therapeutic agents in this category. Its study, however, adds to the body of knowledge on SERMs, potentially aiding in the development of more effective drugs in the future.
References
- ↑ Maximov, P. Y., Lee, T. M., & Jordan, V. C. (2013). The discovery and development of selective estrogen receptor modulators (SERMs) for clinical practice. Current Clinical Pharmacology, 8(2), 135-155.
- ↑ Smith, C. L., & O'Malley, B. W. (2004). Coregulator function: a key to understanding tissue specificity of selective receptor modulators. Endocrine Reviews, 25(1), 45-71.
- ↑ Riggs, B. L., & Hartmann, L. C. (2003). Selective estrogen-receptor modulators — mechanisms of action and application to clinical practice. New England Journal of Medicine, 348(7), 618-629.
Transform your life with W8MD's budget GLP-1 injections from $125.
W8MD offers a medical weight loss program to lose weight in Philadelphia. Our physician-supervised medical weight loss provides:
- Most insurances accepted or discounted self-pay rates. We will obtain insurance prior authorizations if needed.
- Generic GLP1 weight loss injections from $125 for the starting dose.
- Also offer prescription weight loss medications including Phentermine, Qsymia, Diethylpropion, Contrave etc.
NYC weight loss doctor appointments
Start your NYC weight loss journey today at our NYC medical weight loss and Philadelphia medical weight loss clinics.
- Call 718-946-5500 to lose weight in NYC or for medical weight loss in Philadelphia 215-676-2334.
- Tags:NYC medical weight loss, Philadelphia lose weight Zepbound NYC, Budget GLP1 weight loss injections, Wegovy Philadelphia, Wegovy NYC, Philadelphia medical weight loss, Brookly weight loss and Wegovy NYC
|
WikiMD's Wellness Encyclopedia |
| Let Food Be Thy Medicine Medicine Thy Food - Hippocrates |
Medical Disclaimer: WikiMD is not a substitute for professional medical advice. The information on WikiMD is provided as an information resource only, may be incorrect, outdated or misleading, and is not to be used or relied on for any diagnostic or treatment purposes. Please consult your health care provider before making any healthcare decisions or for guidance about a specific medical condition. WikiMD expressly disclaims responsibility, and shall have no liability, for any damages, loss, injury, or liability whatsoever suffered as a result of your reliance on the information contained in this site. By visiting this site you agree to the foregoing terms and conditions, which may from time to time be changed or supplemented by WikiMD. If you do not agree to the foregoing terms and conditions, you should not enter or use this site. See full disclaimer.
Credits:Most images are courtesy of Wikimedia commons, and templates, categories Wikipedia, licensed under CC BY SA or similar.
Contributors: Prab R. Tumpati, MD
