ANTI NEOPLASTIC AGENTS
“STEROIDS & HORMONES”

Content

• Structure, Therapeutic Use, Mechanism of Action of Dromostanolone

• Structure, Therapeutic Use, Mechanism of Action of MEGESTROL

I. DROMOSTANOLONE

• It is a synthetic anabolic steroid that has antiestrogenic effects.

• It is related to dihydrotestosterone.

14-hydroxy-2,4,15-trymethyl tetracyclo-heptadecan-5-one.

Therapeutic Use of DROMOSTANOLONE:

• It is marketed as Drostanolone propionate and its use has been restricted to treatment of metastatic carcinoma of breast.

Mechanism of Action of DROMOSTANOLONE:

• It interacts with the Androgen receptor and modifies gene transcription in presence of co-activators and co-repressors, including increased protein synthesis (anabolism) and decreased amino acid degradation (catabolism).

• It also induces a reduction or inhibition of prolactin or estrogen receptors in the breasts, which indicates anti tumour effects.

II. MEGESTROL

• It is a synthetic derivative of progesterone with antiestrogenic activity.

• 17-acetyl-17-hydroxy-6,10,13-trimethyl-2,8,9,11,12,14,15,16-octahydro-1H-cyclopenta[a]phenanthren-3-one.

Mechanism of Action of MEGESTROL:

• Megestrol binds to and activates nuclear receptors which subsequently bind to and activate target genes for transcription.

• As an antiestrogen, this agent may inhibit the growth-stimulating effects of estrogen on estrogen-sensitive tumor cells.

• Antitumour activity may involve suppression of luteinizing hormone by inhibition of pituitary function.

• In addition, megestrol stimulates appetite in cachectic subjects.

Therapeutic Uses of MEGESTROL:

• It is marketed as Megestrol acetate and is indicated for the palliative treatment of advanced carcinoma of the breast or endometrium.

• Megestrol acetate Oral Suspension USP is indicated for the treatment of anorexia, cachexia, or an unexplained, significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS). 

SUMMARY

• Dromostanolone is a synthetic anabolic steroid that has antiestrogenic effects used in the treatment of breast cancer.

• It acts by binding to the Androgen receptor thereby generating cascade of genetic changes.

• Megestrol is a synthetic derivative of progesterone with antiestrogenic activity used in the treatment of breast and endometrium cancer.

• It acts by inhibiting the growth-stimulating effects of estrogen on estrogen-sensitive tumor cells.