Full Description
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.
Contents
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-β-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 PI3Kδ inhibitor for treating activated PI3Kδ syndrome
15. Leritrelvir (RAY1216): a novel α-ketoamide based peptidomimetic inhibitor of SARS-CoV-2 main protease for COVID-19 treatment
16. Belzutifan: a first-in-class oral HIF-2α 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
