Arostanil

Arostanil Uses, Dosage, Side Effects, Food Interaction and all others data.

Arostanil is an oral steroidal aromatase inhibitor used in the adjuvant treatment of hormonally-responsive (also called hormone-receptor-positive, estrogen-responsive) breast cancer in postmenopausal women. It irreversibly binds to the active site of the enzyme resulting in permanent inhibition.

Aromatase is an enzyme that converts hormones to estrogen in the body's adrenal glands. The aromatase inhibitors (AIs) are drugs that reduce estrogen levels by blocking the action of aromatase in the adrenal glands. The selective AIs (SAIs) selectively reduce levels of estrogen without interfering with levels of other steroid hormones that are produced by the adrenal gland. Drugs in this class include anastrozole (Arimidex ™), letrozole (Femara ™) and exemestane (Aromasin ™).

Trade Name Arostanil
Availability Prescription only
Generic Exemestane
Exemestane Other Names Exemestane, Exemestano, Exemestanum
Related Drugs Arimidex, Ibrance, Femara, Aromasin, Faslodex, Verzenio, Afinitor, Xeloda, Herceptin, Lynparza
Type
Formula C20H24O2
Weight Average: 296.4034
Monoisotopic: 296.177630012
Protein binding

90% (mainly α1-acid glycoprotein and albumin)

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country Lithuania, Romania
Last Updated: September 19, 2023 at 7:00 am
Arostanil
Arostanil

Uses

Arostanil is an aromatase inhibitor used to treat breast cancer in postmenopausal women after treatment with tamoxifen.

For the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy.

Arostanil is also used to associated treatment for these conditions: Early Breast Cancer, Refractory, advanced Breast cancer

How Arostanil works

Breast cancer cell growth may be estrogen-dependent. Aromatase (exemestane) is the principal enzyme that converts androgens to estrogens both in pre- and postmenopausal women. While the main source of estrogen (primarily estradiol) is the ovary in premenopausal women, the principal source of circulating estrogens in postmenopausal women is from conversion of adrenal and ovarian androgens (androstenedione and testosterone) to estrogens (estrone and estradiol) by the aromatase enzyme in peripheral tissues. Estrogen deprivation through aromatase inhibition is an effective and selective treatment for some postmenopausal patients with hormone-dependent breast cancer. Arostanil is an irreversible, steroidal aromatase inactivator, structurally related to the natural substrate androstenedione. It irreversibly binds to the active site causing permanent inhibition necessitating de novo synthesis to restore enzymatic function. Arostanil significantly lowers circulating estrogen concentrations in postmenopausal women, but has no detectable effect on the adrenal biosynthesis of corticosteroids or aldosterone. This reduction in serum and tumor concentrations of estrogen delays tumor growth and disease progression. Arostanil has no effect on other enzymes involved in the steroidogenic pathway up to a concentration at least 600 times higher than that inhibiting the aromatase enzyme.

Toxicity

Convulsions

Food Interaction

  • Take with food. The manufacturer recommends administration following a meal.

Arostanil Disease Interaction

Moderate: osteoporosis, vitamin D deficiency

Elimination Route

42%

Half Life

24 hours

Innovators Monograph

You find simplified version here Arostanil

http://classyfire.wishartlab.com/tax_nodes/C0000000
http://classyfire.wishartlab.com/tax_nodes/C0000012
http://classyfire.wishartlab.com/tax_nodes/C0000258
http://classyfire.wishartlab.com/tax_nodes/C0003568
http://classyfire.wishartlab.com/tax_nodes/C0001467
http://classyfire.wishartlab.com/tax_nodes/C0002973
http://classyfire.wishartlab.com/tax_nodes/C0003558
http://classyfire.wishartlab.com/tax_nodes/C0002977
http://classyfire.wishartlab.com/tax_nodes/C0003487
http://classyfire.wishartlab.com/tax_nodes/C0003940
http://classyfire.wishartlab.com/tax_nodes/C0004150
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:4953
http://www.hmdb.ca/metabolites/HMDB0015125
http://www.genome.jp/dbget-bin/www_bget?drug:D00963
http://www.genome.jp/dbget-bin/www_bget?cpd:C08162
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=60198
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508243
https://www.chemspider.com/Chemical-Structure.54278.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50398447
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=258494
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=4953
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1200374
https://zinc.docking.org/substances/ZINC000003973334
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000625
http://www.pharmgkb.org/drug/PA449563
https://www.ebi.ac.uk/pdbe-srv/pdbechem/chemicalCompound/show/EXM
http://www.rxlist.com/cgi/generic3/exemest.htm
https://www.drugs.com/cdi/exemestane.html
https://en.wikipedia.org/wiki/Exemestane
*** Taking medicines without doctor's advice can cause long-term problems.
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