Xuedong Dai

• Led drug discovery project teams across global R&D sites and external collaborators. Supervised internal employees to build up productive teams. Ensured the smooth communication and efficient performance of CRO resource • Effective multidisciplinary interaction with Computational Chemistry, Biology, DMPK, Toxicology, and CMC at various stages of preclinical small molecule drug discovery from committed to target, HTS follow-up, hit identification/expansion, hit to lead, lead optimization, and IND enabling studies through SAR study with breakthrough in compound potency, selectivity, DMPK and toxicity profiles • Designed analog compounds with diverse pharmacological fingerprints in order to generate multiple chemical series to maximize PoS and expand IP for different therapeutic potentials • Worked with biologists to streamline the flow of preclinical activities by generating screening cascades with stringent progression criteria in all areas of preclinical development (e.g. physicochemical properties, in vitro pharmacology, DMPK profile, Toxicity, etc.)

• Co-inventor of clinical candidate XP23829, a prodrug of Fumaric acid ester, as a potential treatment for patients with moderate-to-severe chronic plaque-type psoriasis and/or relapsing forms of Multiple Sclerosis • Led chemistry projects for the development of prodrugs of Fumaric acid esters (for psoriasis and relapsing MS) and prodrugs of agonists for NMDA receptor (for Schizophrenia and other related CNS disorders). Responsibilities included design and synthesis of novel prodrugs, selection of candidates based on the results of their in vitro DMPK profile, and coordination of efforts to evaluate the candidates in the in vivo studies • Collaborated with analytical department to identify and synthesize impurities to determine the RF values and contributed to the impurity profile for API materials and product formulations of Horizant®/Regnite® • Performed computational studies of the binding modes of A2A and A2B Adenosine Receptor antagonists

• Contributed to medicinal chemistry program that has led to marketed drug Horizant®/Regnite® (a prodrug of Gabapentin) for the treatment of Restless Legs Syndrome and Post-herpetic neuralgia (PHN, a type of neuropathic pain) and the clinical candidate arbaclofen placarbil (XP19986, a prodrug of Baclofen) for the treatment of gastroesophageal reflux disease (GERD) and for the symptoms of spasticity • Developed key strategies to synthesize acyloxyalkyl prodrugs and chirally pure diastereomeric acyloxyalkyl prodrugs, which was applied successfully to the production of API materials for Horizant®/Regnite® and arbaclofen placarbil (XP19986) • Co-inventor of clinical candidate XP21279, a prodrug of L-DOPA, for a potential treatment of Parkinson's disease • Chemistry project leader in charge of the development of prodrugs of L-DOPA and their suitable salts for product formulations • Led the SAR study of derivatives of Mustard compounds as transporter substrates for anticancer program and collaborated with animal facility groups for the in vivo efficacy studies • Led the design and synthesis of prodrugs of Bisphosphonate for the treatment of osteoporosis

• Designed and synthesized focused libraries using liquid-phase combinatorial chemistry • Led optimization for collaborative projects with large pharmaceutical companies (such as J&J, AstraZeneca, etc.) • Co-developed new protecting strategies for catechols and catecholamines

• Led the SAR study of Fumagillin modification to evaluate the anti-angeogenesis properties of its derivatives • Designed and synthesized FK-506 conjugates for a yeast three-hybrid system for detecting ligand-receptor interactions • Solid-phase synthesis of an RGD containing cyclic pentapeptide cyclo(-Arg-Gly-Asp-D-Phe-Lys-), a highly potent and selective inhibitor for the αvβ3 integrin, and therefore an anticancer drug candidate with antiangiogenic properties

• Designed and synthesized chiral atropisomeric quinazolinone phosphine ligands and applied the ligands to Asymmetric allylic alkylation catalyzed by their palladium complexes • Led discussions and gave review lectures in introductory organic chemistry • Supervised students on chemical reactions and operation of modern analytical instruments in both introductory and advanced organic chemistry lab classes • Participated in MIT Chemistry Outreach Program to perform simple and interesting chemical experiments to local high school students to kinder their interests in Chemistry

• Designed and synthesized chiral monomers and monomers with liquid-crystal side chains. Performed the copolymerization of these two types of monomers and studied the optical properties of the resulting copolymers