Monday, February 16, 2015

Anastrozole

Common name: Anastrozole; Anastrozol; Arimidex
Trademarks:  Arimidex
Molecular Formula: C17H19N5 
CAS Registry Number: 120511-73-1
CAS Name: 2-[3-(1-cyano-1-methylethyl)-5-(1H-1,2,4-triazol-1-ylmethyl)phenyl]-2-methylpropanenitrile
Molecular Weight: 293.366
SMILES: CC(C)(C#N)C1=CC(=CC(CN2C=NC=N2)=C1)C(C)(C)C#N
InChI Key: YBBLVLTVTVSKRW-UHFFFAOYSA-N
InChI: InChI=1S/C17H19N5/c1-16(2,9-18)14-5-13(8-22-12-20-11-21-22)6-15(7-14)17(3,4)10-19/h5-7,11-12H,8H2,1-4H3
Activity: Antineoplastic Agents, Hormonal Therapy; Aromatase Inhibitors; Breast Cancer Therapy; Post Surgery Therapy; Estrogen Therapy
Status: Launched 1995
Originator: AstraZeneca

Anastrozole synthesis: US4935437A (also Ref. 2)
Anastrozole synthesis: US20060189670A1

References:
1. Edwards, P. N.; et. al. (Substituted aralkyl) heterocyclic compounds. US4935437A
2. Prous, J., et. al. Drugs Fut 1995, 20, 30-32.
3. Khile, A.; et. al. Process for the preparation of anastrozole and intermediates thereof. US20060189670A1
4. Howell, A.; et. al. Results of the ATAC (Arimidex, Tamoxifen, Alone or in Combination) trial after completion of 5 years’ adjuvant treatment for breast cancer. Lancet 2005, 365(9453), 60-62. (activity)
5. Gangadhara, S.; et. al. Long-term efficacy and safety of anastrozole for adjuvant treatment of early breast cancer in postmenopausal women. Ther Clin Risk Manag 2009, 5(4), 291-300. (activity)