Delving into the Latest Updates on Nilutamide with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

5,5-Dimethyl-3-(α,α,α-trifluoro-4-nitro-m-tolyl)hydantoin, Anandron, Nilutamide (USAN/INN)

+ [3]

Target

AR

Action

antagonists

Mechanism

AR antagonists(Androgen Receptor antagonists)

Therapeutic Areas

NeoplasmsUrogenital Diseases

Active Indication

Prostatic Cancer

Inactive Indication-

Originator Organization-

Active Organization

Sanofi

Roussel

Advanz Pharma Corp. Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

France (01 Jan 1987),

Prostatic Cancer

Regulation-

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Structure/Sequence

Molecular FormulaC12H10F3N3O4

InChIKeyXWXYUMMDTVBTOU-UHFFFAOYSA-N

CAS Registry63612-50-0

This is a prospective, open-label, multi-center seamless phase II to phase III randomized clinical trial designed to compare SST with or without PET-directed local therapy in improving the castration-resistant prostate cancer-free survival (CRPC-free survival) for Veterans with oligometastatic prostate cancer. Oligometastasis will be defined as 1-10 sites of metastatic disease based on the clinical determination of the LSI which incorporates all imaging, clinical, and pathologic data available.

Start Date01 Jul 2021

Sponsor / Collaborator

VA Office of Research and Development

NCT03678025

/ RecruitingPhase 3IIT

Phase III Randomized Trial of Standard Systemic Therapy (SST) Versus Standard Systemic Therapy Plus Definitive Treatment (Surgery or Radiation) of the Primary Tumor in Metastatic Prostate Cancer

This phase III trial studies how well standard systemic therapy with or without definitive treatment (prostate removal surgery or radiation therapy) works in treating participants with prostate cancer that has spread to other places in the body. Addition of prostate removal surgery or radiation therapy to standard systemic therapy for prostate cancer may lower the chance of the cancer growing or spreading.

Start Date24 Sep 2018

Sponsor / Collaborator

National Cancer Institute

CTRI/2018/01/011386

/ CompletedPhase 1

A randomized, open label, multi-center, two-treatment, two-period, two-sequence, two-waycross-over, multiple dose, steady state Bioequivalence (BE) study of Genus Lifesciences Inc.Nilutamide Tablets 150 mg with NILANDRONÂ® (Nilutamide) Tablets 150 mg from ConcordiaPharmaceuticals Inc. in metastatic prostate cancer patients. - NLM101

Start Date01 Mar 2018

Sponsor / Collaborator

Genus Lifesciences, Inc.

100 Clinical Results associated with Nilutamide

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100 Translational Medicine associated with Nilutamide

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100 Patents (Medical) associated with Nilutamide

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579

Literatures (Medical) associated with Nilutamide

04 Feb 2025·Open Medicine

Lathyrol affects the expression of AR and PSA and inhibits the malignant behavior of RCC cells

Article

Author: Jiang, Junling ; Zhao, Junfeng ; Zhou, Lei ; Tai, Lunwei ; Song, Shengyou

AbstractObjectiveTo investigate how lathyrol affects aggressive behaviors and related proteins of the androgen receptor (AR) 786-O cells.Methods786-O cells were cultured in vitro and divided into these groups at random: the dimethylsulfoxide (DMSO) control group (A group), negative control group (B group), and experimental group (C group). Cells in A group were grown in DMSO working medium (contained RPMI 1640 medium and 1% DMSO), B group cells were cultured in nilutamide working medium (contained DMSO working medium and 325 μg/mL nilutamide), while those in C group were cultured in lathyrol working medium (contained DMSO working medium and 300 μg/mL lathyrol). Cell proliferation was measured via CCK-8 assays, and cell apoptosis was examined through terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling staining. Scratch tests and Transwell invasion tests were used to evaluate cell movement and penetration. The expression information about p-AR, AR, p-Akt, ki67, caspase3, cleaved-caspase3, Bcl-2, Bax, caspase9, cleaved-caspase9, and GAPDH proteins was investigated through western blotting. Immunocytochemistry was used to identify the 786-O cells’ secretion level of matrix metalloproteinase 2 (MMP2), MMP9, and prostate-specific antigen (PSA) proteins.ResultsThe negative control and experimental groups’ cells exhibited reduced proliferation, migration, and invasion and increased apoptosis after 24 h treatment. Furthermore, these two group cells exhibited a notable reduction in the status of Ki67, Bcl-2, MMP2, MMP9, and p-Akt (P < 0.05) and significantly increased the expressions of AR, p-AR, Bax, cleaved-caspase3, and cleaved-caspase9 (P < 0.05). There was no statistical distance in PSA, caspase3, and caspase9 expressions among the three groups (P > 0.05).ConclusionIn vitro, lathyrol and nilutamide exert notable anticancer effects by effectively suppressing the proliferation, migration, and invasion of 786-O cells while also inducing apoptosis.

01 Feb 2025·Food Chemistry

Fabrication of MnSnO2 intercalated TA-rGO modified sensor for selective electrochemical detection of chloramphenicol in real samples

Article

Author: Selvi, Subash Vetri ; Hsiao, Wesley Wei-Wen ; Alagumalai, Krishnapandi ; Krishnapandi, Alagumalai

Chloramphenicol (CAP), a potent antibiotic capable of inhibiting protein synthesis, presents significant challenges related to long-term dosing and its persistent leaching into the environment, raising concerns about environmental contamination and resistance development. To address this issue, we developed a reliable, low-cost, and biocompatible nanocomposite material comprising tannic acid (TA)-reduced graphene oxide (rGO) intercalated into manganese-doped tin oxide nanoparticles (MnSnO₂ NPs). The structural formation and catalytic activity of the MnSnO₂ NPs/TA-rGO nanocomposite were characterized using field emission-scanning electron microscopy (FE-SEM), high-resolution transmission electron microscopy (HR-TEM), X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FT-IR), Raman spectroscopy, X-ray photoelectron spectroscopy (XPS), and electrochemical techniques. This material exhibits robust interfacial interactions and synergistic effects, resulting in an admirable electrocatalytic reduction response for CAP sensing. The presence of co-interference molecules improved the selectivity performance of the MnSnO₂ NPs/TA-rGO-modified glassy carbon electrode. The fabricated exhibited a two linear determination range (0.011-103.43 μmol L^-1 and 103.43-1924.16 μmol L^-1), with a detection limit (LOD) is 6.7 nmol L^-1 and limit of quantification (LOQ) is 12.3 nmol L^-1. Furthermore, this sensor demonstrated good sensitivity, admirable reproducibility, repeatability, and storage stability. Finally, the practicability of the fabricated MnSnO₂ NPs/TA-rGO glassy carbon electrode sensor was evaluated by analyzing the CAP content in milk, honey, eye drops, biofluids (human serum and urine), and river water, and satisfactory recovery rates of 95.4 %-100.3 % were noted.

10 Jan 2025·Mini-Reviews in Medicinal Chemistry

Recent Development in Hydantoins, Thiohydantoins, and Selenohydantoins as Anticancer Agents: Structure-activity Relationship and Design Strategies

Article

Author: Jain, Sanmati Kumar ; Thakur, Gajendra Singh ; Gupta, Ajay Kumar

Hydantoin, a five-membered heterocyclic scaffold, is regarded as a crucial scaffold in medicinal chemistry. Hydantoins have been useful in synthesizing medicines like nilutamide, enzalutamide, and apalutamide. Thiohydantoin and selenohydantoin have been discovered as two separate types of hydantoin. There are two hydrogen bond donors, two hydrogen bond acceptors, and four substitution sites. These characteristics have led to the design, synthesis, and expansion of hydantoin derivatives' biological and pharmacological effects against numerous types of malignancies. This study reviews the recent contributions of hydantoin and its isosteric variants to medicinal chemistry. To emphasize their significance, certain significant compounds based on hydantoins and their structure activity relationships (SAR) are briefly discussed. We thoroughly analyzed each scaffolds' structural characteristics and SAR, and these scaffolds may one day show potential anticancer activities.

1

News (Medical) associated with Nilutamide

04 Apr 2013

·covispharma.com

Covis Pharma to Acquire U.S. Rights from Sanofi for Nilandron®, Plaquenil®, Rilutek®, Uroxatral®, and Kayexalate®

ZUG, Switzerland, April 4, 2013 /PRNewswire/ -- Covis Pharma Sarl ("Covis Pharma"), a Switzerland-based specialty pharmaceutical company today announced an agreement with sanofi-aventis U.S. LLC and certain of its affiliates ("Sanofi") to acquire full commercial rights for Nilandron® (nilutamide), Plaquenil® (hydroxychloroquine), Rilutek® (riluzole), Uroxatral® (alfuzosin hydrochloride), and Kayexalate® (sodium polystyrene sulfate) in the United States. The aggregate sales for these products in the United States in 2012 were $114.6 million. Sanofi will retain the existing rights for these products in countries outside the United States. Terms of the agreement have not been disclosed. "We are very pleased to announce the addition of these products to our existing portfolio," said Jack Davis, CEO of Covis Pharma. "Covis will continue to supply consistent, top quality, branded pharmaceuticals, ensuring that patients receive the therapeutic care they need." Covis Pharma will promote these branded products through its US-based distributor, Covis Pharmaceuticals Inc. Covis Pharma also supplies authorized generic products to the US market through a separate distributor, Rising Pharmaceuticals Inc. Sanofi will manufacture and supply the products for Covis Pharma. The agreement has received Hart-Scott-Rodino regulatory clearance in the United States. About Covis Pharma Headquartered in Zug, Switzerland, Covis Pharma is a global specialty pharmaceutical company providing therapeutic solutions to patients. The company's distinctive product portfolio addresses life threatening and other serious medical conditions. With eleven branded products currently in market, Covis Pharma aims to become a leading specialty pharmaceutical company through organic, as well as global acquisitive, growth. The investor group in Covis Pharma has significant investment and operational experience in the specialty pharmaceutical industry. Led by affiliates of Cerberus Capital Management, L.P., one of the world's leading private investment firms, the investor group also includes Princeton Biopharma Capital Partners, LLC and Bourne Partners. For more information, visit www.covispharma.com. Inquiries: Covis Pharma, 212-891-1558, info@covispharma.com SOURCE Covis Pharma

License out/inDrug Approval

100 Deals associated with Nilutamide

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External Link

KEGG	Wiki	ATC	Drug Bank
D00965	Nilutamide	L02BB02	DB00665

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Prostatic Cancer	Colombia	Sanofi	-
Prostatic Cancer	Venezuela	Sanofi	-

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Prostatic Cancer	Phase 2	Peru	Sanofi	-
Prostatic Cancer	Phase 2	Peru	Sanofi	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00918385 (ARS, CTgov)	Phase 2	Metastatic castration-resistant prostate cancer	57	Nilutamide (Arm 1=High AR Nilutamide)	(zkayvcsolx) = ompnuiyepx ilpihmpkdv (ioybgkhpek, rotkpmiutl - ikzucqkhxm) View more	-	29 Oct 2014
NCT00918385 (ARS, CTgov)	Phase 2	Metastatic castration-resistant prostate cancer	57	Dasatinib+Nilutamide (Arm 2= Low AR Dasatinib)	(zkayvcsolx) = qmbyhajrgu ilpihmpkdv (ioybgkhpek, hoprtlcuca - oewwbndtap) View more	-	29 Oct 2014
NCT00028769 (S0032, CTgov)	Phase 2	Metastatic Prostate Carcinoma	41	etoposide+estramustine+paclitaxel+bicalutamide+flutamide+leuprolide acetate+goserelin acetate+nilutamide	(myfwzyzkkh) = eupdortbwm ehmvkucezt (nbtvealbmk, funuuilyuh - vzeqkmqixv) View more	-	16 Jul 2013
NCT00020254 (Pubmed \| Clin Cancer Res)	Phase 2	Castration-Resistant Prostatic Cancer	-	Vaccine	rtjxpqyfxb(npcwpewrap) = wrgvcomiub stxcwwslqv (otfsmdjhvj )	-	15 Jul 2008
NCT00020254 (Pubmed \| Clin Cancer Res)	Phase 2	Castration-Resistant Prostatic Cancer	-	Nilutamide	rtjxpqyfxb(npcwpewrap) = xhhtkklctt stxcwwslqv (otfsmdjhvj )	-	15 Jul 2008
ASCO2007	Not Applicable	Non-metastatic prostate cancer	-	Nilutamide	(rlylnwmikt) = hbpmlowbkk trixydkbhb (rlfzlerwpp )	-	20 Jun 2007
ASCO2005	Not Applicable	Castration-Resistant Prostatic Cancer	45	Nilutamide	bxoyiefjdi(jgpyvxcwfv) = The most common reversible adverse effects were mild to moderate visual adaptation alterations (20%) nyaliapxoa (sfznzcqvqo )	Positive	01 Jun 2005