Vincent Njar


Njar Group



Call: (240) 314-6448


  • Postdoctoral Fellow, Worcester Foundation for Experimental Biology, Shrewsbury, MA, 1980-1982
  • Ph.D., Organic Chemistry, University College London/University of London, United Kingdom, 1980
  • B.S., Chemistry, University of Ibadan, Nigeria 1976


Dr. Vincent Njar has a long-standing interest in the rational discovery and development of small molecules as anti-cancer agents. He is a leading medicinal chemist and oncopharmacologist who has made significant discoveries in the development of novel small molecules with potential for the treatment of a variety of cancers – in particular, breast, prostate, and pancreatic cancers. Dr. Njar invented novel chemical reactions for the synthesis of novel inhibitors of a number of important anti-cancer targets. He is perhaps best known for his development of RAMBAs – retinoic acid metabolism blocking agents, and the molecule Galeterone, which is commercially available as a unique research reagent.


Novel RAMBA Retanamides

RAMBAs work by inhibiting an enzyme called all-trans retinoic acid (ATRA) metabolism enzyme (also known as CYP26). Some of the Njar group’s original RAMBAs compounds are potent inhibitors of breast and prostate cancer cell growth in vitro, and strong inhibitors of breast and prostate cancer tumors in animal xenograft models.

In ongoing studies, the Njar lab has discovered that novel retinamides (NRs) also antagonize transactivation of the androgen receptor (AR), and degrade the full-length and splice variant ARs in human prostate cancer cell lines. In addition, the NRs exquisitely cause degradation of MAP kinase-interacting kinases (Mnk1 and 2). This blocks initiation of eukaryotic translation initiation factor 4E (eIF4E) cap-dependent translation in both human breast and prostate cancer cell lines, promoting apoptosis and impeding cell growth, cell proliferation, and matrix invasion of breast and prostate cancer cell lines. To the best of the lab’s knowledge, its NRs are the first Mnk1/2 degraders known, making them strong candidates for development as novel anti-breast/prostate cancer therapeutics. The Njar lab’s lead Mnk1/2 degrader is called VNLG-152.  Further development of these agents is ongoing in collaboration with Isoprene Pharmaceuticals, Inc., a small business founded by Dr. Njar in July 2018.

Next-Generation Galeterone Analogs

In collaboration with the late Dr. Angela Brodie, internationally renowned breast cancer researcher, Njar developed some of the most potent known inhibitors of prostate cancer target protein CYP17. The lead clinical candidate, Galeterone (formerly called VN/124-1 or TOK-001), successfully advanced through Phase I and II studies under an exclusive license by the University of Maryland, Baltimore to Tokai Pharmaceuticals, Inc. Galeterone was well tolerated, with promising clinical activity in men with castration-resistant prostate cancer. However, the Phase III trial, ARMOR3-SV, was unsuccessful; efforts to rescue Galeterone are ongoing.

Efforts in the Njar Lab are ongoing to discover and develop next-generation Galeterone analogs (NGGAs). Njar’s group has demonstrated that Galeterone and NGGAs also degrade Mnk1/2, causing inhibition of tumor growth, metastasis, and treatment resistance in various cancers. Gratifyingly, the lead NGGAs, also called Galnex small-molecules, have superior efficacies and pharmaceutical properties compared to Galeterone. The lab’s lead Galnex is called VNPP433-3β.


VNLG-152R and its deuterated analogs potently inhibit/repress triple/quadruple negative breast cancer of diverse racial origins in vitro and in vivo by upregulating E3 Ligase Synoviolin 1 (SYVN1) and inducing proteasomal degradation of MNK1/2.
Salinization Dramatically Enhance the Anti-Prostate Cancer Efficacies of AR/AR-V7 and Mnk1/2 Molecular Glue Degraders, Galeterone and VNPP433-3β Which Outperform Docetaxel and Enzalutamide in CRPC CWR22Rv1 Xenograft Mouse Model.
Targeted Degradation of Androgen Receptor by VNPP433-3β in Castration-Resistant Prostate Cancer Cells Implicates Interaction with E3 Ligase MDM2 Resulting in Ubiquitin-Proteasomal Degradation.
Murine Toxicology and Pharmacokinetics of Lead Next Generation Galeterone Analog, VNPP433-3β.
Novel AR/AR-V7 and Mnk1/2 Degrader, VNPP433-3β: Molecular Mechanisms of Action and Efficacy in AR-Overexpressing Castration Resistant Prostate Cancer In Vitro and In Vivo Models.
Large-scale synthesis of galeterone and lead next generation galeterone analog VNPP433-3β.
Novel deuterated Mnk1/2 protein degrader VNLG-152R analogs: Synthesis, In vitro Anti-TNBC activities and pharmacokinetics in mice.
Transcriptome profiling reveals that VNPP433-3β, the lead next-generation galeterone analog inhibits prostate cancer stem cells by downregulating epithelial-mesenchymal transition and stem cell markers.
Prospects for Clinical Development of Stat5 Inhibitor IST5-002: High Transcriptomic Specificity in Prostate Cancer and Low Toxicity In Vivo.
Galeterone and The Next Generation Galeterone Analogs, VNPP414 and VNPP433-3β Exert Potent Therapeutic Effects in Castration-/Drug-Resistant Prostate Cancer Preclinical Models In Vitro and In Vivo.
A Quality Improvement Approach to Increase Exercise Assessment in Survivors of Childhood Leukemia.
The Novel Mnk1/2 Degrader and Apoptosis Inducer VNLG-152 Potently Inhibits TNBC Tumor Growth and Metastasis.
Structure of the Fc fragment of the NIST reference antibody RM8671.
Submultiple Data Collection to Explore Spectroscopic Instrument Instabilities Shows that Much of the "Noise" is not Stochastic.
Quantitative analysis of the impact of a human pathogenic mutation on the CCT5 chaperonin subunit using a proxy archaeal ortholog.
Characterization of the NISTmAb Reference Material using small-angle scattering and molecular simulation : Part I: Dilute protein solutions.
The retinamide VNLG-152 inhibits f-AR/AR-V7 and MNK-eIF4E signaling pathways to suppress EMT and castration-resistant prostate cancer xenograft growth.
Novel galeterone analogs act independently of AR and AR-V7 for the activation of the unfolded protein response and induction of apoptosis in the CWR22Rv1 prostate cancer cell model.
Short-chained oligo(ethylene oxide)-functionalized gold nanoparticles: realization of significant protein resistance.
Biophysical characterization and structure of the Fab fragment from the NIST reference antibody, RM 8671.