Physical Properties Colour : Light yellow solid

Molecular Weight : 623.64 g·mol−1

Melting Point : 204 0C
Odour : No data available
Mechanism of Action The mechanism of action of relugolix is as a Gonadotropin Releasing
Hormone Receptor Antagonist, and Cytochrome P450 3A Inducer, and
Cytochrome P450 2B6 Inducer, and Breast Cancer Resistance Protein
Inhibitor, and P-Glycoprotein Inhibitor. The physiologic effect of
relugolix is by means of Decreased GnRH Secretion.
The pathogenesis and progression of
prostate cancer appear driven, at least in
part, by the effects of
testosterone.5 Androgen deprivation has
been demonstrated to result in cell death and
tumor regression in many well-differentiated
prostate cancer cell lines - for this reason,
androgen deprivation therapy (ADT) has
become a standard in the treatment of
prostate cancer, particularly in advanced
disease
Testosterone production in males is carried
out in the Leydig cells of testes and is
stimulated by luteinizing hormone (LH),
which itself is produced in the pituitary gland
following the binding of gonadotropin-
releasing hormone (GnRH) to corresponding
GnRH receptors.11 Relugolix is a competitive
antagonist of these GnRH receptors, thereby
decreasing the release of LH and, ultimately,
testosterone

Pharmacokinetic
Dosage
Dosage Forms & Strengths
tablet
 120mg
Prostate Cancer
Indicated for advanced prostate cancer
Day 1 loading dose: 360 mg PO
Maintenance dose: 120 mg PO qDay
Dosage Modifications
Renal impairment
 Mild-to-severe (CrCl 15-89 mL/min): No
dosage adjustment required
 End-stage renal disease with or without
hemodialysis: Not studied
Hepatic impairment
NAME :- SAMARTH SUNIL MUDAKE
ROLL NO : - 81

1) : (Brand Name : - ) Rolugolix