Rohan K Rej

Top skills:
· Drug Design • Synthetic Organic Chemistry • Drug Discovery • Organic Synthesis • Medicinal Chemistry

Executive Summary:
· Dynamic, visionary, and self-motivated drug hunter with 10 years of experience in drug discovery at the University of Michigan.
· Highly successful medicinal and synthetic organic chemist with a proven track record of making impactful contributions and solving problems across multiple projects, collaborating with teams in diverse disease areas.
· Possesses extensive scientific, technical, analytical, and interpretive skills, along with practical laboratory experience in experimental design, execution, and integrated data analysis, all crucial for the success of drug discovery programs.
· Strong background in synthetic and medicinal chemistry, demonstrated by significant contributions to development candidates in oncology, with the most advanced compound (APG-5918) successfully reaching Phase 1 clinical trials.
· Over 5 years of experience managing and supervising overseas contract research organizations (CROs) to efficiently deliver high-quality, results-focused test compounds for biological evaluation.
· Solid publication record as the lead or corresponding author on the majority of scientific papers, patents, and presentations at both internal and external scientific meetings.

My research focuses on organic synthesis and its application in modern medicine. As a researcher, my efforts are directed towards a multidisciplinary approach, which involves using organic and medicinal chemistry and computational tools to design and achieve desired small molecules that can be used as new cancer therapeutics. Currently, we are developing inhibitors and degraders of various targets, which are crucial in cancer treatment. We have made significant progress in this area, and we are optimistic that our research will positively impact the lives of cancer patients.
Inhibitors and degraders of the following targets are in progress or accomplished.
1. SMARCA degrader and ‘Precision ADCs’ for SMARCA protein: Cells with a mutated SMARCA4 are dependent on the related helicase SMARCA2 for their survival, which positions SMARCA2 as an ideal target for synthetic lethality-based therapies. While there has been the discovery of inhibitors that act on the ATPase activities of both SMARCA2 and SMARCA4, the lack of selectivity and resultant toxicity in both animal studies and human clinical trials limit their therapeutic use. Additionally, identified inhibitors of the bromodomains of SMARCA2 and SMARCA4 failed to impact cancer cell viability, which indicates a need for more effective therapeutic strategies that target SMARCA2 selectively in SMARCA4-mutated cancers. Currently, I am playing a critical role in discovering SMARCA degrader and ‘Precision ADCs’ for SMARCA protein. My aim is to expand the reach of SMARCA degraders to cancers beyond those with SMARCA4 mutations. The current work was published in Journal of Medicinal Chemistry (J. Med. Chem. 68(2): 1113–1133).
2. Estrogen Receptor PROTACs: ERD-12310A and ERD-1233, two highly potent and orally bioavailable estrogen receptor heterobifunctional PROTACs. These compounds are designed for the treatment of ER+/HER2− locally advanced or metastatic breast cancer. They demonstrated strong ERα degradation in vitro, excellent oral bioavailability in rodents, and superior antitumor efficacy in MCF-7 xenograft models, including those harboring the resistance-associated ESR1Y537S mutation. These results were published in the Journal of Medicinal Chemistry (J. Med. Chem. 2024, 67, 23, 20933–20965; J. Med. Chem. 67(21): 19010–19037).
3. IKZF2 Degrader: PVTX-405 is a selective molecular glue degrader targeting IKZF2 while sparing IKZF1 and IKZF3. This compound showed robust in vivo degradation of IKZF2 and demonstrated promising immunomodulatory activity. In preclinical models, PVTX-405 outperformed anti-PD1 therapy in tumor suppression and showed translational potential in both non-human primates and patients. These findings were published in Nature Communications (Nat Commun. 16(1): 4095, May 2025).
4. Development of the clinical candidate for EED inhibitors: (EEDi-5273/ APG-5918, ClinicalTrials.gov Identifier: NCT05415098; NCT05773586). Phase I study is in progress both in US and China in patients with in advanced solid tumors or lymphomas and anemic patients. These results were published in the Journal of Medicinal Chemistry (J. Med. Chem. 2021, 64, 19, 14540-14556, J. Med. Chem. 2020, 63, 13, 7252-7267).
5. Design and development of AR PROTAC for patients with Metastatic Castration-Resistant Prostate Cancer (mCRPC). The compound is in the advanced stage of preclinical development.
6. Structure-based design, synthesis, and SAR studies of small-molecule inhibitors and degraders of LSD1. The compound is in the advanced stage of preclinical development.
These results were published in the ACS Med. Chem. Lett. 2023, 14, 1389–1395.