U.S.-based Nigerian doctor wins award for discoveries on cancer

A United States (U.S.) based Nigerian doctor; Prof. Vincent Njar, has won the David J. Ramsay Entrepreneur of the Year Award for his novel discoveries on possible cures for cancer.

Njar, a professor at the Department of Pharmacology, University of Maryland School of Medicine (UMSOM), US, has already had a significant impact in the fight against cancer. Could finding a cure lie in his future?

According to the report published by UMSOM on its website https://www.umaryland.edu/founders/founders-week-award-winners, Njar, an internationally respected medicinal chemist and oncopharmacologist who is head of the medicinal chemistry section in the Center for Biomolecular Therapeutics (CBT) at the Institute for Bioscience and Biotechnology Research, UMSOM, focuses his research and inventions on the discovery and development of small molecules as anti-cancer agents. His work has led to the development of novel therapeutics for breast, prostate, and pancreatic cancers — some of the most prevalent and deadly cancers.

He has taken those discoveries a step further by founding two companies over the years that have helped him to direct the early development of his inventions and technologies, leading him to be named the University of Maryland, Baltimore’s (UMB) 2021 David J. Ramsay Entrepreneur of the Year.

“Being an entrepreneur means to undertake a high-risk, high-reward venture and be fearless in the process. Over the years, I have realized that entrepreneurship means doing, doing, doing until something useful or impactful gets made,” Njar said. “I believe in what I am doing, and I am not afraid to ask for help. Being a successful entrepreneur requires thorough planning, creativity, and hard work.”

Njar’s most significant discoveries include retinoic acid metabolism blocking agents (RAMBAs), or novel retinamides (NRs), that inhibit the growth of breast and prostate cancer cells and tumors. The NRs he discovered cause degradation of mitogen-activated protein (MAP) kinase-interacting kinases (Mnk1 and 2), which can promote tumor progression.

After closing his first startup, Terpene Pharmaceuticals, LLC, in 2018, he partnered with UMB’s New Ventures Initiative to found Isoprene Pharmaceuticals, Inc. (IPI), an early-stage small molecule oncology company developing oral therapeutics for triple negative breast cancer and other cancers.

Njar, who is IPI’s chief executive officer, said the company is focused on oncology applications of the NRs developed in his laboratory.

“To the best of my knowledge, our NRs are the first Mnk1 and 2 degraders known, making them strong candidates for development as novel anti-breast/prostate cancer therapeutics,” he said. “Further development of these agents is ongoing in collaboration with IPI.”

IPI was recently awarded a two-year, approximately $2 million Small Business Innovation Research grant from the National Cancer Institute (NCI) for a translational project to develop a novel therapeutic for triple negative breast cancer.

In addition to cancer, these protein degraders have applications in dermatology, inflammatory bowel disorders, and other diseases. IPI has recently partnered with Hoth Therapeutics, Inc. to develop their use in dermatology and inflammatory bowel disorders.

Njar also has worked on the design, discovery, and clinical translation of Galeterone, a novel CYP17 inhibitor/androgen receptor-degrading agent for the treatment of cancer. Galeterone was licensed by Tokai Pharmaceuticals, Inc. and advanced to Phase 3 clinical trials showing dramatic activity in men with hormone refractory metastatic prostate cancer. Because of its clinical efficacy, Galeterone and subsequent variants continue to be developed as novel therapeutics for prostate and pancreatic cancers.

“I am relentlessly pursuing the development of Galeterone technology toward commercial success and medical impact,” Njar said. “For example, two clinical trials were initiated just this year based on recent preclinical studies from my lab. Specifically, we demonstrated that Galeterone impedes pancreatic cancer cell migration, invasion, and proliferation and inhibits tumor growth in mice.”

The work has led to a Phase 2 clinical trial at the University of Maryland Marlene and Stewart Greenebaum Comprehensive Cancer Center (UMGCCC). The Galeterone technology has been licensed to LTN Pharmaceuticals, Inc., which is continuing its clinical development.

“This trial is highly anticipated since Galeterone remains a potent orally available molecule that has now been shown to inhibit prostate cancer growth in patients with castration-resistant prostate cancer,” said David J. Weber, PhD, professor, Department of Biochemistry and Molecular Biology, UMSOM, and director, CBT.

Njar’s most recent National Institutes of Health (NIH) R01 grant focuses on the development of next-generation Galeterone analogs for prostate cancer. He also received a two-year NIH/NCI award to support prostate cancer disparity collaborative research.

“Dr. Njar is one of the most accomplished medicinal chemists of any cancer center in the United States,” said Kevin J. Cullen, MD, Marlene and Stewart Greenebaum Distinguished Professor in Oncology, UMSOM, and director, UMGCCC. “What is particularly remarkable about Dr. Njar’s contributions is that he has developed numerous novel compounds, which have rapidly moved into clinical testing and are showing enormous promise as important cancer therapeutics.”

Margaret M. McCarthy, PhD, James and Carolyn Frenkil Dean’s Professor, and chair, Department of Pharmacology, UMSOM, agreed.

“The rapidity with which Vincent’s discoveries have been employed in clinical trials serves as a testament to the unmet need of novel therapeutics in oncology and the relevance of his studies,” she said.

Njar has secured 34 issued patents, more than 30 pending patents, and numerous active intellectual property and licensing activities at UMB.

Weber said Njar’s accomplishments are rare.
“Very few investigators see their discoveries translated from basic science discovery into a clinical study in their lifetime, let alone multiple times within their career, as is the case with Dr. Njar,” he said. “I find that Dr. Njar is a highly creative scientist who turns his ideas into tangible scientific, therapeutic, and medically impactful accomplishments. He truly has a knack for pursuing the synthesis and development of molecules with extraordinary anti-cancer activities.”

Njar came to UMSOM in 1999 and worked with cancer research pioneer Angela Brodie, MD, to develop aromatase inhibitors for the treatment of postmenopausal breast cancer. Njar, who was named an inaugural Distinguished University Professor by UMB, said working with Brodie helped him develop his mentoring skills.

“Through collaboration with Dr. Brodie, I was able to acquire astute knowledge of cancer biology and oncopharmacology,” he said. “This enabled me to train 11 PhDs in molecular medicine/life sciences, many postdoctoral fellows, and research associates who have all proceeded to reputable positions in academia, industry, and government.”

Cullen called Njar “the heir” to Brodie’s legacy. “Like her, he has been able to synthesize novel compounds, develop them in preclinical models, and lead them rapidly into the clinic. Dr. Njar’s work has the potential to impact cancer patients around the world,” he said.

Njar said receiving the phone call from UMB President Bruce E. Jarrell, MD, FACS, telling him he had been named Entrepreneur of the Year was “one of the best days of my life.”

“The award is very encouraging and has energized me to keep plugging on,” he said. “I am optimistically cautious that my entrepreneurship will eventually produce at least one U.S. Food and Drug Administration-approved anti-cancer drug for the benefit of mankind.”

Njar received his. B.Sc. (Hons.) from University of Ibadan (UI), Nigeria in Chemistry in 1976, and his Ph.D. from University College London, United Kingdom in Organic and Medicinal Chemistry in 1980. His postdoctoral training with the late Dr. Eliahu Caspi was at the Worcester foundation for Experimental Biology, Shrewsbury, Massachusetts, US (1980-1982).

He joined the faculty at UI as Lecturer II in 1982. He was promoted through the ranks and became Professor of Organic Chemistry in 1996. During his tenure at UI, he was visiting professor at several institutions, including: Johns Hopkins University, Baltimore, USA (1988, 1989, 1992 & 1993); Universite de Sherbrooke, Sherbrooke, Quebec, Canada (1990); University of Southampton, Southampton, UK (1991, 1992 & 1995); and University of Saarland, Saarbruecken, Germany (1994-1995). During these research visits he collaborated with eminent scholars including: Professors Cecil Robinson (Johns Hopkins), Liat Tan (Sherbrooke), Muhammad Akhtar (Southampton) and Rolf Hartmann (Saarland). Theses research visits were made possible by grant and fellowship awards from US National Institutes of Health, Bethesda, USA; International Union Against Cancer, Geneva, Switzerland; Medical Research Council of Canada; Alexander von Humboldt Foundation, Bonn, Germany and Wellcome Trust Foundation, London, UK.

Following several research visits from 1996 to 1998 collaborating with Dr. Angela Brodie at University of Maryland, Baltimore (UMB), he was appointed Assistant Professor of Pharmacology in 1999 and was promoted to Associate Professor in 2002. In 2008, Dr. Njar was appointed Professor of Medicinal Chemistry and Oncopharmacology at Jefferson School of Pharmacy, Thomas Jefferson University, Philadelphia, PA, US. Finally, in January 2012, he came back to UMB as Professor of Medicinal Chemistry and Pharmacology and Head, Medicinal Chemistry Section of the newly established Center for Biomolecular Therapeutics (CBT).