NILANDRON- nilutamide tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

Nilutamide (UNII: 51G6I8B902) (Nilutamide - UNII:51G6I8B902)

Available from:

Concordia Pharmaceuticals Inc.

INN (International Name):

Nilutamide

Composition:

Nilutamide 150 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

NILANDRON tablets are indicated for use in combination with surgical castration for the treatment of metastatic prostate cancer (Stage D2 ). For maximum benefit, NILANDRON treatment must begin on the same day as or on the day after surgical castration. NILANDRON tablets are contraindicated: - in patients with severe hepatic impairment (baseline hepatic enzymes should be evaluated prior to treatment) - in patients with severe respiratory insufficiency - in patients with hypersensitivity to nilutamide or any component of this preparation.

Product summary:

NILANDRON 150 mg tablets are supplied in boxes of 30 tablets. Each box contains 3 child-resistant, PVC, aluminum foil-backed blisters of 10 tablets (NDC 59212-111-14). Each white, biconvex, cylindrical (10 mm in diameter) tablet has a triangular logo on one side and an internal reference number (168D) on the other. Store at 25°C (77°F); excursions permitted between 15-30°C (59-86°F) [see USP Controlled Room Temperature]. Protect from light. Keep out of reach of children. Rev. 09/19 Mfd. for: Concordia Pharmaceuticals Distributed by: Amdipharm Limited 17 Northwood House Dublin 9, Ireland © 2015 All rights reserved.

Authorization status:

New Drug Application

Summary of Product characteristics

NILANDRON - NILUTAMIDE TABLET
CONCORDIA PHARMACEUTICALS INC.
----------
NILANDRON
(NILUTAMIDE)
TABLETS
DESCRIPTION
NILANDRON tablets contain nilutamide, a nonsteroidal, orally active
antiandrogen
having the chemical name
5,5-dimethyl-3-[4-nitro-3-(trifluoromethyl)phenyl]-2,4-
imidazolidinedione with the following structural formula:
Nilutamide is a microcrystalline, white to practically white powder
with a molecular weight
of 317.25. Its molecular formula is C
H
F N O .
It is freely soluble in ethyl acetate, acetone, chloroform, ethyl
alcohol, dichloromethane,
and methanol. It is slightly soluble in water [<0.1% W/V at 25°C
(77°F)]. It melts
between 153°C and 156°C (307.4°F and 312.8°F).
Each NILANDRON tablet contains 150 mg of nilutamide. Other ingredients
in
NILANDRON tablets are corn starch, lactose, povidone, docusate sodium,
magnesium
stearate, and talc.
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
Prostate cancer is known to be androgen sensitive and responds to
androgen ablation.
In animal studies, nilutamide has demonstrated antiandrogenic activity
without other
hormonal (estrogen, progesterone, mineralocorticoid, and
glucocorticoid) effects. In
vitro, nilutamide blocks the effects of testosterone at the androgen
receptor level. In
vivo, nilutamide interacts with the androgen receptor and prevents the
normal
androgenic response.
PHARMACOKINETICS
_Absorption:_
®
®
12
10 3
3
4
_Absorption:_
Analysis of blood, urine, and feces samples following a single oral
150-mg dose of [
C]-
nilutamide in patients with metastatic prostate cancer showed that the
drug is rapidly
and completely absorbed and that it yields high and persistent plasma
concentrations.
_Distribution:_
After absorption of the drug, there is a detectable distribution
phase. There is moderate
binding of the drug to plasma proteins and low binding to
erythrocytes. The binding is
nonsaturable except in the case of alpha-1-glycoprotein, which makes a
minor
contribution to the total concentration of proteins in the plasma. The
results of binding
s