1971 - Development of first aromatase inhibitor 4-OHA used in treatment of breast cancer.
Pharmacology; Women's Health
About This Innovation
* In 1971 Brodie joined her husband's lab as staff scientist, moving into breast cancer research. They were researching its link with estrogen and an enzyme that produces it, aromatase. * They developed several steroidal aromatase inhibitors, with Brodie focused on 4-OHA. * Following further clinical trials, 4-OHA, named Formestane, was the first aromatase inhibitor used on breast cancer patients and proved to be a significant improvement on tamoxifen, the standard cancer drug used to treat estrogen receptor-positive breast cancer in postmenopausal women. * The drug was first marketed in 1994.
The Invention
Ester derivatives of 4-hydroxy-4-androstene-3 17-dione & a method for inhibiting estrogen biosynthesis; C-4 substituted retinoids; C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens in vitro biological activities pharmacokinetics & antitermor activity; 17-azolyl steroids useful as androgen synthesis inhibitors; Compositions & methods of inducing endoplasmic reteculum stress response for the treatment of cell proliferative diseases; Androgen synthesis inhibitors; 20-substituted pregnene derivatives & their use as androgen synthesis inhibitors; HDAC inhibitors & hormone targeted drugs for the treatment of cancer; Prodrugs of C-17-heteroarlyl steroidal CYP17 inhibitors/antiandrogens:synthesis in vitro biological activities pharmacokinetics & antitumor activity
Key Information
Category:
Pharmacology; Women's Health
Completion Status:
done
Patent Number:
4235893;7265143;10098896;6444683;6200965;5994335;8785423;6133280;5264427;5994334;8110550;9295679;7875599;90181198
Co-Inventor:
Harry J. Brodie; David A. Marsh; Vincent C.O. Njar; Ivo P. Nnane; Robert Bruno; Yangzhi Ling; Jisong Li; Gauri Sabnis; Lalji Gediya
Patent Information
Patent Number: 4235893;7265143;10098896;6444683;6200965;5994335;8785423;6133280;5264427;5994334;8110550;9295679;7875599;90181198
Technical Specifications
Ester derivatives of 4-hydroxy-4-androstene-3 17-dione & a method for inhibiting estrogen biosynthesis; C-4 substituted retinoids; C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens in vitro biological activities pharmacokinetics & antitermor activity; 17-azolyl steroids useful as androgen synthesis inhibitors; Compositions & methods of inducing endoplasmic reteculum stress response for the treatment of cell proliferative diseases; Androgen synthesis inhibitors; 20-substituted pregnene derivatives & their use as androgen synthesis inhibitors; HDAC inhibitors & hormone targeted drugs for the treatment of cancer; Prodrugs of C-17-heteroarlyl steroidal CYP17 inhibitors/antiandrogens:synthesis in vitro biological activities pharmacokinetics & antitumor activity
Collaboration
Co-Inventor: Harry J. Brodie; David A. Marsh; Vincent C.O. Njar; Ivo P. Nnane; Robert Bruno; Yangzhi Ling; Jisong Li; Gauri Sabnis; Lalji Gediya