Drug Discovery Stories, Volume Two showcases the discovery journeys of recent blockbuster drugs approved between 2023 and 2024, along with promising drug candidates. This book delves into structural biology, biological functions of targets, hit compound identification, hit-to-lead optimization, binding modes, key biological and pharmacokinetic data, and clinical results. It also covers other candidate compounds against the same targets and includes additional content based on the authors' choices. The series addresses the rapid evolution in drug discovery and development, appealing to those in chemical biology, synthetic chemistry, and pharmacology.
By highlighting interdisciplinary collaboration, the authors plan to release updated editions every few years to ensure the content reflects the latest achievements and breakthroughs in the field.
1. Daprodustat (GSK-1278863): A Small Molecule Hypoxia Inducible Factor
(HIF)-Prolyl Hydroxylase Inhibitor for Anemia
2. Repotrectinib (TPX-0005): a macrocyclic ALK/ROS1/TRK inhibitor for the
treatment of non-small cell lung cancer
3. FRUZAQLA (fruquintinib): a selective oral inhibitor of VEGFR -1, -2 and -3
for treating for adults with metastatic colorectal cancer
4. Ensitrelvir: an orally active 3C-like protease inhibitor for COVID-19.
5. Danuglipron: Pioneering Oral GLP1 Receptor Agonists Paving the Way for
Revolutionizing Diabetes Treatment
6. Remdesivir: An Early Repurposed RNA-Dependent RNA Polymerase Inhibitor for
Treating COVID-19
7. RNK05047: A chaperone-mediated protein degrader that selectively targets
BRD4 while recruiting the HSP90 chaperone
8. Risdiplam: an Orally Active Survival Motor Neuron (SMN2) pre-mRNA Splicing
Modifier for Spinal Muscular Atrophy (SMA) in pediatric and adult patients
9. Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and
Metallo--lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections
10. Etrasimod: a selective sphingosine-1-phosphate (S1P) receptor modulator
for the treatment of ulcerative colitis
11. NX-5948: an BTK degrader in Ph. Ia/Ib for patients with advanced B-cell
malignancies
12. Omaveloxolone (RTA-408): an NRF2 activator for Friedreich's ataxia
13. Azvudine: a reverse transcriptase inhibitor for AIDS and COVID-19
treatment
14. Leniolisib: a potent and selective PI3K inhibitor for treating activated
PI3K syndrome
15. Leritrelvir (RAY1216): a novel -ketoamide based peptidomimetic inhibitor
of SARS-CoV-2 main protease for COVID-19 treatment
16. Belzutifan: a first-in-class oral HIF-2 inhibitor approved for patients
with Von Hippel-Landau (VHL) disease-associated renal cell carcinoma
17. Sotagliflozin: a Dual SGLT1/2 Inhibitor, for Full Range of Heart Failure
18. Fezolinetant: the first FDA-approved NK3 receptor antagonist for treating
moderate-to-severe vasomotor symptoms associated with menopause
19. Gepirone: a selective partial agonist of the 5-HT1A Receptor in the
treatment of Depression
20. Aducanumab: A Milestone in Alzheimer's Disease Treatment Targeting
Amyloid Beta Plaques
21. Varoglutamstat (PQ912): Navigating the Frontiers of Alzheimer's
Treatment
22. Lequembi: Pioneering Hope in Neurodegenerative Disorders - A Breakthrough
Drug Shaping the Future of Treatment
Professor Bin Yu obtained his PhD degree from Zhengzhou University and University of Cambridge and currently is a professor of medicinal chemistry at School of Pharmaceutical Sciences, Zhengzhou University. His research interests focus on chemistry driven drug discovery for novel therapeutics. To date, he has published over 120 papers in international high-impact peer-reviewed journals including Journal of Medicinal Chemistry, Organic Letters, Pharmacology & Therapeutics, Journal of Hematology & Oncology, Drug Discovery Today, Acta Pharmaceutica Sinica B, etc., 10 of them were published in journal with impact factor (IF) >10. Peng Zhan obtained his B.S. degree from Shandong University, China, in 2005. He then earned his M.S. and Ph.D. degrees in medicinal chemistry from Shandong University in 2008 and 2010. He subsequently joined Shandong University as a Lecturer (20102012). From 2012 to 2014, he worked as a postdoctoral fellow funded by Japan Society for the Promotion of Science. He is currently a full professor in the Department of Medicinal Chemistry, Shandong University. His research interests involve the discovery of novel anti-viral (HIV, HBV, influenza, coronavirus, etc.), anti-gout, and anti-cancer agents based on rational drug design and combinatorial chemistry approaches. He also co-edited six books published by People's Medical Publishing House and Springer Nature, respectively and granted 50 patents (30 of them licensed). He currently serves as advisory editorial board member of Journal of Medicinal Chemistry.
