ATC Group: L02B Hormone antagonists and related agents

The World Health Organization's ATC classification organizes medical drugs based on therapeutic properties, chemical composition, and anatomy. It helps make essential medicines readily available globally and is widely used in the pharmaceutical industry.

Position of L02B in the ATC hierarchy

Level Code Title
1 L Antineoplastic and immunomodulating agents
2 L02 Endocrine therapy
3 L02B Hormone antagonists and related agents

Group L02B contents

Code Title
L02BA Anti-estrogens
L02BB Anti-androgens
L02BG Aromatase inhibitors
L02BX Other hormone antagonists and related agents

Active ingredients in L02B

Active Ingredient Description
Abarelix

Abarelix is a synthetic decapeptide and antagonist of naturally occurring gonadotropin-releasing hormone (GnRH). Abarelix binds to and blocks the gonadotropin releasing hormone receptor in the anterior pituitary gland, thereby inhibiting the secretion and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. Abarelix is primarily used in oncology to reduce the amount of testosterone made in patients with advanced symptomatic prostate cancer for which no other treatment options are available.

Abiraterone

Abiraterone acetate is converted in vivo to abiraterone, an androgen biosynthesis inhibitor. Specifically, abiraterone selectively inhibits the enzyme 17α-hydroxylase/C17,20-lyase (CYP17). This enzyme is expressed in and is required for androgen biosynthesis in testicular, adrenal and prostatic tumour tissues. CYP17 inhibition also results in increased mineralocorticoid production by the adrenals.

Anastrozole

Anastrozole is a potent and highly selective non-steroidal aromatase inhibitor. It inhibits the enzyme aromatase, which is responsible for converting androgens to estrogens. Anastrozole is a drug indicated in the treatment of breast cancer in post-menopausal women.

Apalutamide

Apalutamide is an orally administered, selective Androgen Receptor (AR) inhibitor that binds directly to the ligand-binding domain of the AR. Apalutamide treatment decreases tumor cell proliferation and increases apoptosis leading to potent antitumor activity.

Bicalutamide

Bicalutamide is a non-steroidal antiandrogen, devoid of other endocrine activity. It binds to androgen receptors without activating gene expression, and thus inhibits the androgen stimulus. Regression of prostatic tumours results from this inhibition.

Darolutamide

Darolutamide is an androgen receptor (AR) inhibitor with a flexible polar-substituted pyrazole structure that binds with high affinity directly to the receptor ligand binding domain. Darolutamide competitively inhibits androgen binding, AR nuclear translocation, and AR mediated transcription. Darolutamide treatment decreases prostate tumour cell proliferation leading to potent antitumour activity.

Degarelix

Degarelix is a selective gonadotrophin releasing-hormone (GnRH) antagonist that competitively and reversibly binds to the pituitary GnRH receptors, thereby rapidly reducing the release of the gonadotrophins, luteinizing hormone (LH) and follicle stimulating hormone (FSH), and thereby reducing the secretion of testosterone (T) by the testes.

Elacestrant

Elacestrant, a tetrahydronaphthalene compound, is a potent, selective and orally active estrogen receptor-α (ERα) antagonist and degrader. Elacestrant inhibits the estradiol-dependent and independent growth of ERα-positive breast cancer cells, including models harbouring estrogen receptor 1 (ESR1) gene mutations.

Enzalutamide

Enzalutamide is a potent androgen receptor signalling inhibitor that blocks several steps in the androgen receptor signalling pathway. Enzalutamide treatment decreases the growth of prostate cancer cells and can induce cancer cell death and tumour regression.

Exemestane

Exemestane is an irreversible, steroidal aromatase inhibitor, structurally related to the natural substrate androstenedione.

Flutamide

Flutamide is a non-steroidal, highly specific, orally active anti-androgenic agent. The pharmacologically active metabolite, hydroxyflutamide, is believed to exert an anti-androgenic effect directly on the target tissues, either by inhibiting androgen uptake or by blocking cytoplasmic and nuclear binding of androgen. Flutamide is indicated for the treatment of advanced prostatic carcinoma in which suppression of testosterone effects is indicated.

Formestane
Fulvestrant

Fulvestrant is a competitive estrogen receptor (ER) antagonist with an affinity comparable to estradiol. Fulvestrant blocks the trophic actions of estrogens without any partial agonist (estrogen-like) activity.

Letrozole

Letrozole is a non-steroidal aromatase inhibitor. It inhibits the aromatase enzyme by competitively binding to the haem of the aromatase cytochrome P450, resulting in a reduction of oestrogen biosynthesis in all tissues where present.

Nilutamide
Relugolix

Relugolix is a nonpeptide GnRH receptor antagonist that competitively binds to GnRH receptors in the anterior pituitary gland preventing native GnRH from binding and signalling the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). Consequently, the production of testosterone from the testes is reduced.

Tamoxifen

Tamoxifen is a non-steroidal, triphenylethylene-based drug which displays a complex spectrum of oestrogen antagonist and oestrogen agonist-like pharmacological effects in different tissues.

Toremifene

Toremifene is a nonsteroidal triphenylethylene derivative that binds to estrogen receptors and may produce estrogenic, anti-estrogenic or both effects, depending upon the duration of treatment, animal species, gender, target organ and variable selected. Toremifene is indicated in first line hormone treatment of hormone-dependent metastatic breast cancer in postmenopausal patients.

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