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

Mechanism

AR antagonists(Androgen Receptor antagonists)

Therapeutic Areas

NeoplasmsUrogenital Diseases

Active Indication

Prostatic Cancer

Inactive Indication-

Originator Organization-

Active Organization

SanofiConcordia Pharmaceuticals, Inc.

Roussel

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

FR (01 Jan 1987),

Prostatic Cancer

Regulation-

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Structure

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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275

Literatures (Medical) associated with Nilutamide

08 Nov 2024·ACS Infectious Diseases

Single-Dose Drug Development Candidate for Schistosomiasis

Article

Author: Charman, Susan A. ; Campbell, Michael ; Pham, Thao ; Shackleford, David M. ; Patil, Rahul ; Jones, Jeremy O. ; Davis, Paul H. ; Vennerstrom, Jonathan L. ; Keiser, Jennifer ; Hu, Meiyu ; Wang, Xiaofang ; Neville, Andrew J. ; Katneni, Kasiram ; Häberli, Cécile ; Schulze, Thomas T. ; Leas, Derek A. ; Dong, Yuxiang ; Chen, Gong

Aryl hydantoins were identified in the early 1980s as a promising antischistosomal chemotype. However, as exemplified by Ro 13-3978, this compound series produced antiandrogenic side effects on the host, a not unexpected outcome given their structural similarity to the antiandrogenic drug nilutamide. The two key advances in our optimization of Ro 13-3978 were swapping the aryl trifluoromethyl substituent with a difluoroethyl to abolish antiandrogenic effects and replacing the hydrogen atoms of the gem-dimethyl substructure with deuterium atoms to increase metabolic stability. Combining these two structural changes led to the discovery of single-dose drug candidate AR102, a compound with potent, selective, and broad-spectrum activity against schistosomes, a long pharmacokinetic half-life in preclinical species, and an acceptable safety profile.

01 Feb 2024·Computational Biology and Chemistry

Targeting AR-positive breast cancer cells via drug repurposing approach

Article

Author: Sen, Plaboni ; Ghosh, Siddhartha Sankar ; Dutta, Parijat ; Kandasamy, Thirukumaran

Androgen Receptor (AR) is overexpressed in almost all the molecular subtypes of breast cancer. Besides aiding the tumorigenic environment of cancer by abnormal cell proliferation, AR also takes part in promoting cancer signaling pathways, thereby promoting aggressiveness. In this study, AR was selected as the target protein in breast cancer cells. Following this, a library of 1293 FDA-approved drugs was screened via molecular docking, MD simulation, and MMPBSA binding energy. Amongst the library of compounds, Adapalene exhibited the least binding energy of (-10.2 kCal/mol) in comparison to that of the chosen reference compound, Nilutamide (-8.6 kCal/mol). Furthermore, the in vitro efficacy of Adapalene was also determined in two different breast cancer cell lines such as MCF7 (AR-positive/ER-positive) and MDA-MB-231 (AR negative/TNBC). Initially, the cell viability assay (MTT) was performed, which endowed us with a lesser IC₅₀ value of Adapalene in comparison to Nilutamide in both cell lines. The IC₅₀ of Adapalene was found to be 12 μM and 39.4 μM in MCF7 and MDA-MB-231 cells, respectively. Furthermore, Adapalene also induced cellular ROS and apoptosis by 3.5-fold and 26.58% in MCF7 cells. However, the overall effect of Adapalene was significantly lower in the case of MDA-MB-231 cell lines, which could be attributed to its inherent nature of the absence of hormone receptors. Conclusively, Adapalene possesses greater therapeutic efficacy in comparison to the control drug, thereby hinting towards the potential use of Adapalene in the treatment of AR-positive breast cancer.

01 Sep 2023·Prostate international

Oral chemotherapeutic agents in metastatic hormone-sensitive prostate cancer: A network meta-analysis of randomized controlled trials.

Article

Author: Chang, In Ho ; Tae, Jong Hyun ; Kim, Jin Wook ; Choi, Joongwon ; Choi, Se Young ; Nguyen, Tuan Thanh ; Kim, Seong Hwan ; Myung, Soon Chul ; Kim, Tae-Hyoung ; Lee, Yong Seong ; Kim, Jung Hoon ; Kim, Myoungsuk

BackgroundMultiple oral chemotherapeutic agents for metastatic hormone-sensitive prostate cancer (mHSPC) have been developed for conjugated use with conventional androgen deprivation therapy (ADT). Several randomized controlled trials (RCTs) report significant benefits in mHSPC patients. Therefore, we compared overall survival (OS) and progression-free survival (PFS) benefits among considerable mHSPC oral chemotherapeutic agents.Materials and methodsWe investigated mHSPC treatment efficacy through a systematic RCT-trial literature review (PubMed, Embase, Web of Science, the Cochrane Library, and Scopus). Two reviewers independently screened, extracted data, and assessed bias risk in duplicate.ResultsWe identified 18 RCTs (n = 13,509). Concerning OS, ADT + abiraterone, ADT + abiraterone + docetaxel, ADT + apalutamide, ADT + bicalutamide, ADT + darolutamide + docetaxel, ADT + enzalutamide, ADT + orteronel, and ADT + rezvilutamide were more effective than the standard of care (SOC). Comparing PFS, most treatments were more effective than SOC, excluding ADT + bicalutamide, nilutamide, flutamide, ADT + bicalutamide + palbociclib, and ADT + nilutamide. ADT + docetaxel with androgen receptor targeted agent (ARTA) triplet therapy was not among the top three treatments determined through ranking analysis.ConclusionsNovel oral chemotherapeutic agent combination therapies must replace current ADT monotherapy and ADT + docetaxel SOC. Even so, ADT + docetaxel with ARTA triplet therapy still is not the best mHSPC treatment and requires further study.

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	CO	Sanofi	-
Prostatic Cancer	VE	Sanofi	-

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Prostatic Cancer	Phase 3	PE	Sanofi	-
Prostatic Cancer	Phase 1	PE	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)	(zeeglgmjxz) = vhiwgzmevm shlbgwwseh (bjlpeefsvr, jhyxhperaw - mxszyqtbgp) View more	-	29 Oct 2014
NCT00918385 (ARS, CTgov)	Phase 2	Metastatic castration-resistant prostate cancer	57	Dasatinib+Nilutamide (Arm 2= Low AR Dasatinib)	(zeeglgmjxz) = ebtoiwvmss shlbgwwseh (bjlpeefsvr, nqkcjjiqnk - klrwipjsft) View more	-	29 Oct 2014
NCT00028769 (S0032, CTgov)	Phase 2	Metastatic Prostate Carcinoma	41	etoposide+estramustine+paclitaxel+bicalutamide+flutamide+leuprolide acetate+goserelin acetate+nilutamide	tlbpcjqhup(spbnmnyetr) = xsamdinwnn lryttmjlpx (nwcszyfymr, scuweplhcj - bseeayhysk) View more	-	16 Jul 2013
NCT00020254 (Pubmed \| Clin Cancer Res)	Phase 2	Castration-Resistant Prostatic Cancer	-	Vaccine	(proozypjai) = daajjouyfk bbsmjhusbs (cjrjimtqqr )	-	15 Jul 2008
NCT00020254 (Pubmed \| Clin Cancer Res)	Phase 2	Castration-Resistant Prostatic Cancer	-	Nilutamide	(proozypjai) = ydyidalkqh bbsmjhusbs (cjrjimtqqr )	-	15 Jul 2008
ASCO2007	Not Applicable	Non-metastatic prostate cancer	-	Nilutamide	(kztclaqfat) = khzbsgvqfp zwxbsunxbj (eitaqcuvbz )	-	20 Jun 2007
ASCO2005	Not Applicable	Castration-Resistant Prostatic Cancer	45	Nilutamide	zdmuwfirrb(fjkzigdyik) = The most common reversible adverse effects were mild to moderate visual adaptation alterations (20%) igeewdbvis (inmuyaqzmb )	Positive	01 Jun 2005