Investigational Drug Details
| Drug ID: | D357 |
| Drug Name: | Anastrozole |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB01217 |
| DrugBank Description: | Anastrozole is a non-steroidal aromatase inhibitor (AI), similar to [letrozole], used to decrease circulating estrogen levels in the treatment of postmenopausal women with estrogen-responsive breast cancer.[L8863] Anastrozole is also related to [exemestane], a steroidal AI, but its non-steroidal nature provides stark advantages including a lack of steroid-associated adverse effects such as weight gain and acne.[A186865] Aromatase inhibitors, including anastrozole, have become endocrine drugs of choice in the treatment of postmenopausal breast cancer due to a more favourable efficacy and adverse effect profile as compared to earlier estrogen receptor modulators such as [tamoxifen].[A186877,A186955] Anastrozole was first approved for use in the United States in 1995.[L8863] |
| PubChem ID: | 2187 |
| CasNo: | 120511-73-1 |
| Repositioning for NAFLD: | Yes |
| SMILES: | CC(C)(C#N)C1=CC(=CC(CN2C=NC=N2)=C1)C(C)(C)C#N |
| Structure: |
|
| InChiKey: | YBBLVLTVTVSKRW-UHFFFAOYSA-N |
| Molecular Weight: | 293.3663 |
| DrugBank Targets: | Cytochrome P450 19A1 |
| DrugBank MoA: | Anastrazole exerts its anti-estrogenic effects via selective and competitive inhibition of the aromatase enzyme found predominantly in the adrenal glands, liver, and fatty tissues.[A186877] Many breast cancers are hormone receptor-positive, meaning their growth is stimulated and/or maintained by the presence of hormones such as estrogen or progesterone.[L8863] In postmenopausal women, estrogen is primarily derived from the conversion of adrenally-produced androgens into estrogens by the aromatase enzyme - by competitively inhibiting the biosynthesis of estrogen at these enzymes, anastrozole effectively suppresses circulating estrogen levels and, subsequently, the growth of hormone receptor-positive tumours.[A186877,A186958] |
| DrugBank Pharmacology: | Anastrozole prevents the conversion of adrenal androgens (e.g. [testosterone]) to estrogen in peripheral and tumour tissues. As the growth of many breast cancers is stimulated and/or maintained by the presence of estrogen, anastrozole helps to treat these cancers by decreasing the levels of circulating estrogens.[L8869,A186958] Anastrozole has a relatively long duration of action allowing for once daily dosing - serum estradiol is reduced by approximately 70% within 24 hours of beginning therapy with 1mg once daily, and levels remain suppressed for up to 6 days following cessation of therapy.[L8863] The incidence of ischemic cardiovascular events was increased during anastrozole therapy and patients with pre-existing ischemic heart disease should consider the risks and benefits of anastrozole before beginning therapy. Anastrozole has also been reported to decrease spine and hip bone mineral density (BMD), so consideration should be given to monitoring of BMD in patients receiving long-term therapy.[L8863,A186955] |
| DrugBank Indication: | Anastrozole is indicated as adjunct therapy in the treatment of hormone receptor-positive early breast cancer in postmenopausal women, and as a first-line treatment for hormone receptor-positive (or hormone receptor-unknown) locally advanced or metastatic breast cancer in postmenopausal women.[L8863] It may also be used in the treatment of advanced breast cancer in postmenopausal women who experience disease progression despite treatment with [tamoxifen].[L8866,L8863] |
| Targets: | |
| Therapeutic Category: | |
| Clinical Trial Progress: | |
| Latest Progress: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L5111 | NCT02146079 | PHASE1 | COMPLETED | NO | 2014-05-21 | 2018-04-18 | Details |
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
|---|
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Article ID | PMID | Source | Title |
|---|