{"product_id":"chemistry-and-pharmacology-of-drug-discovery-hardback-9781394225125","title":"Chemistry and Pharmacology of Drug Discovery (Hardback) 9781394225125","description":"\u003cfont face=\"Georgia\"\u003e\r\n\u003cp\u003e\u003cfont size=\"6\"\u003eChemistry and Pharmacology of Drug Discovery\u003c\/font\u003e\u003cbr\u003e\r\n\r\n\r\n\r\n\r\n\r\n\u003c\/p\u003e\n\u003cp\u003e\u003cfont size=\"4\"\u003eJie Jack Li (Edited by), JJ Li (Author)\u003c\/font\u003e\u003c\/p\u003e\r\n\r\n\u003cp\u003e\u003cfont size=\"3\"\u003e9781394225125, Wiley\u003c\/font\u003e\u003c\/p\u003e\r\n\r\n\u003cp\u003e\u003cfont size=\"3\"\u003eHardback, published 7 August 2024\u003c\/font\u003e\u003c\/p\u003e\r\n\r\n\u003cp\u003e\u003cfont size=\"3\"\u003e432 pages\u003cbr\u003e25.4 x 17.8 x 2.4 cm, 0.454 kg\u003c\/font\u003e\u003c\/p\u003e\r\n\r\n\r\n\r\n\r\n\r\n\u003cp align=\"justify\"\u003e\u003cstrong\u003e\u003cfont size=\"3\"\u003e\u003cp\u003e\u003cb\u003eCase studies of 20 successful FDA-approved drugs, from biological rationale to clinical efficacy studies and state-of-the-art applications\u003c\/b\u003e \u003c\/p\u003e\n\u003cp\u003e\u003ci\u003eChemistry and Pharmacology of Drug Discovery\u003c\/i\u003e illustrates how chemistry, biology, pharmacokinetics, and a host of disciplines come together to produce successful medicines, discussing a total of 20 drugs that are all FDA-approved post 2021—some of which are first-in-class and revolutionary. \u003c\/p\u003e\n\u003cp\u003eThe four sections in this book cover Infectious Disease, Cancer Drugs, CNS Drugs, and Miscellaneous Drugs. Each chapter covers background material on the drug class and\/or disease indication and key aspects relevant to the discovery of the drug, including structure-activity relationships, pharmacokinetics, drug metabolism, efficacy, and safety. \u003c\/p\u003e\n\u003cp\u003eThis book is contributed to by various veterans and well-known experts in medical chemistry, many of whom discovered the drugs they reviewed, leading to tremendous quality and depth of insight. \u003c\/p\u003e\n\u003cp\u003eSome of the drugs covered in \u003ci\u003eChemistry and Pharmacology of Drug Discovery\u003c\/i\u003e include: \u003c\/p\u003e\n\u003cul\u003e\n\u003cli\u003eNirmatrelvir (Paxlovid with Ritonavir), a 3-chymotrypsin-like protease inhibitor for treating SARS-CoV-2 infection\u003c\/li\u003e\n\u003cli\u003eDoravirine (Pifeltro), a third-generation non-nucleoside reverse transcriptase inhibitor for the treatment of HIV-1 infection\u003c\/li\u003e\n\u003cli\u003eOteseconazole (Vivjoa), a CYP51 inhibitor for treating recurrent vulvovaginal candidiasis, and Rimegepant (Nurtec ODT), a CGRP antagonist for treating migraine\u003c\/li\u003e\n\u003cli\u003eCiprofol (Cipepofol), a γ-Aminobutyric acid receptor agonist for induction of anesthesia, and Ozanimod (Zeposia), an S1P receptor antagonist for treating multiple sclerosis\u003c\/li\u003e\n\u003cli\u003eDeucravacitinib (Sotyktu), a first-in-class deuterated TYK2 inhibitor for the treatment of plaque psoriasis\u003c\/li\u003e\n\u003c\/ul\u003e \u003cp\u003e\u003ci\u003eChemistry and Pharmacology of Drug Discovery\u003c\/i\u003e serves as an excellent and highly authoritative learning resource for medicinal, organic, synthetic, and process chemists as well as research scientists in lead optimization and process development.\u003c\/p\u003e\u003c\/font\u003e\u003c\/strong\u003e\u003c\/p\u003e\r\n\r\n\u003cp\u003e\u003cfont size=\"3\"\u003e\u003cp\u003ePreface xi\u003c\/p\u003e \u003cp\u003eContributing Authors xiii\u003c\/p\u003e \u003cp\u003e\u003cb\u003eSection I. Drugs Treating Infectious Diseases 1\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 1. Nirmatrelvir (Paxlovid with Ritonavir): A 3-Chymotrypsin-like Protease Inhibitor for Treating SARS-CoV-2 Infection 3\u003cbr\u003e \u003c\/b\u003e\u003ci\u003eJie Jack li\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1 Background 4\u003c\/p\u003e \u003cp\u003e2 Pharmacology 5\u003c\/p\u003e \u003cp\u003e2.1 The Coronavirus 5\u003c\/p\u003e \u003cp\u003e2.2 The 3CL Protease 6\u003c\/p\u003e \u003cp\u003e2.3 The Mechanism of Action of Nirmatrelvir 9\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 10\u003c\/p\u003e \u003cp\u003e3.1 The Pyrrolidone Substituent at P\u003csub\u003e1\u003c\/sub\u003e 10\u003c\/p\u003e \u003cp\u003e3.2 Dimethylcyclopropylproline at P\u003csub\u003e2\u003c\/sub\u003e 11\u003c\/p\u003e \u003cp\u003e3.3 The Nitrile Warhead at P\u003csub\u003e1\u003c\/sub\u003e’ 13\u003c\/p\u003e \u003cp\u003e3.4 Lead Optimization 14\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 17\u003c\/p\u003e \u003cp\u003e4.1 Pharmacokinetics of Nirmatrelvir 17\u003c\/p\u003e \u003cp\u003e4.2 Metabolism of Nirmatrelvir 17\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 18\u003c\/p\u003e \u003cp\u003e6 Synthesis 19\u003c\/p\u003e \u003cp\u003e6.1 Scale-up Route 19\u003c\/p\u003e \u003cp\u003e6.2 Manufacturing Route 23\u003c\/p\u003e \u003cp\u003e7 Summary 24\u003c\/p\u003e \u003cp\u003eReferences 25\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 2. Doravirine (Pifeltro): A Third-generation Nonnucleoside Reverse Transcriptase Inhibitor as a Treatment of HIV-1 Infection 29\u003cbr\u003e \u003c\/b\u003e\u003ci\u003eJie Jack li\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1 Background 30\u003c\/p\u003e \u003cp\u003e2 Pharmacology 32\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 38\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 43\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 45\u003c\/p\u003e \u003cp\u003e6 Synthesis 46\u003c\/p\u003e \u003cp\u003e7 Summary 49\u003c\/p\u003e \u003cp\u003eReferences 49\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 3. Cabotegravir (Vocabria): An HIV Integrase Strand Transfer Inhibitor for Treating HIV Infection 53\u003cbr\u003e \u003c\/b\u003e\u003ci\u003eJie Jack li\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1 Background 54\u003c\/p\u003e \u003cp\u003e2 Pharmacology 54\u003c\/p\u003e \u003cp\u003e2.1 HIV Integrase 54\u003c\/p\u003e \u003cp\u003e2.2 First-Generation HIV Integrase Inhibitors 58\u003c\/p\u003e \u003cp\u003e2.3 Second-Generation HIV Integrase Inhibitors 61\u003c\/p\u003e \u003cp\u003e2.4 Integrase–LEDGF\/p75 Allosteric Inhibitors 63\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 65\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 68\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 69\u003c\/p\u003e \u003cp\u003e6 Synthesis 70\u003c\/p\u003e \u003cp\u003e7 Summary 74\u003c\/p\u003e \u003cp\u003eReferences 74\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 4. Lenacapavir (Sunlenca): A Long-acting HIV-1 Capsid Protein Inhibitor for Treating HIV Infection 77\u003cbr\u003e \u003c\/b\u003e\u003ci\u003eJie Jack li\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1 Background 78\u003c\/p\u003e \u003cp\u003e2 Pharmacology 79\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 85\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 89\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 90\u003c\/p\u003e \u003cp\u003e6 Synthesis 90\u003c\/p\u003e \u003cp\u003e7 Summary 95\u003c\/p\u003e \u003cp\u003eReferences 95\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 5. Fostemsavir (Rukobia): An HIV-1 gp120-Direceted Attachment Inhibitor for Treating AIDS 97\u003cbr\u003e \u003c\/b\u003e\u003ci\u003eTao Wang and Xiang li\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1 Background 97\u003c\/p\u003e \u003cp\u003e2 Pharmacology 99\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 100\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 106\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 109\u003c\/p\u003e \u003cp\u003e6 Synthesis 110\u003c\/p\u003e \u003cp\u003e7 Summary 116\u003c\/p\u003e \u003cp\u003eReferences 117\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 6. Oteseconazole (Vivjoa): A CYP51 Inhibitor for Treating Recurrent Vulvovaginal Candidiasis 121\u003cbr\u003e \u003c\/b\u003e\u003ci\u003eCharles L. Lail III and Timothy J. Hagen\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1 Background 121\u003c\/p\u003e \u003cp\u003e2 Pharmacology 130\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 132\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 135\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 136\u003c\/p\u003e \u003cp\u003e6 Synthesis 137\u003c\/p\u003e \u003cp\u003e7 Summary 141\u003c\/p\u003e \u003cp\u003eReferences 141\u003c\/p\u003e \u003cp\u003e\u003cb\u003eSection II. Oncology Drugs 147\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 7. Futibatinib (Lytgobi): A Selective Irreversible FGFR1‒4 Inhibitor 149\u003cbr\u003e \u003c\/b\u003e\u003ci\u003eFaridoon and Guiping Zhang\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1 Background 149\u003c\/p\u003e \u003cp\u003e2 Pharmacology 152\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 154\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 158\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 158\u003c\/p\u003e \u003cp\u003e6 Synthesis 159\u003c\/p\u003e \u003cp\u003e7 Summary 163\u003c\/p\u003e \u003cp\u003eReferences 163\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 8. Pacritinib (Vonjo): A Dual JAK2\/IRAK1 Inhibitor for Treating Myelofibrosis 167\u003cbr\u003e \u003c\/b\u003e\u003ci\u003eFaridoon and Guiping Zhang\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1 Background 167\u003c\/p\u003e \u003cp\u003e2 Pharmacology 169\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 172\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 176\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 178\u003c\/p\u003e \u003cp\u003e6 Synthesis 179\u003c\/p\u003e \u003cp\u003e7 Summary 183\u003c\/p\u003e \u003cp\u003eReferences 183\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 9. Tucatinib (Tukysa): An Oral, Selective HER2 Inhibitor for the Treatment of HER2-positive Solid Tumors 187\u003cbr\u003e \u003c\/b\u003e\u003ci\u003eFengtao Zhou and Ke Ding\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1 Background 188\u003c\/p\u003e \u003cp\u003e2 Pharmacology 189\u003c\/p\u003e \u003cp\u003e3 Pharmacokinetics and Drug Metabolism 190\u003c\/p\u003e \u003cp\u003e4 Efficacy and Safety 191\u003c\/p\u003e \u003cp\u003e5 Synthesis 192\u003c\/p\u003e \u003cp\u003e6 Summary 196\u003c\/p\u003e \u003cp\u003eReferences 197\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 10. Tazemetostat (Tazverik): An EZH2 Inhibitor for Treatment of Epithelioid Sarcoma and Follicular Lymphoma 199\u003cbr\u003e \u003c\/b\u003e\u003ci\u003eRuheng Zhao and Timothy A. Cernak\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1 Background 199\u003c\/p\u003e \u003cp\u003e2 Pharmacology 200\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 202\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 207\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 208\u003c\/p\u003e \u003cp\u003e6 Synthesis 209\u003c\/p\u003e \u003cp\u003e7 Summary 212\u003c\/p\u003e \u003cp\u003eReferences 212\u003c\/p\u003e \u003cp\u003e\u003cb\u003eSection III. CNS Drugs 215\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 11. Ozanimod (Zeposia): An S1P Receptor Modulator for Treating Multiple Sclerosis and Inflammatory Bowel Diseases 217\u003cbr\u003e \u003c\/b\u003e\u003ci\u003eShaohui Yu and Xi Wang\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1 Background 217\u003c\/p\u003e \u003cp\u003e2 Pharmacology 220\u003c\/p\u003e \u003cp\u003e3 Drug Metabolism and Pharmacokinetics 226\u003c\/p\u003e \u003cp\u003e4 Structure–Activity Relationship (SAR) 228\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 232\u003c\/p\u003e \u003cp\u003e6 Synthesis 236\u003c\/p\u003e \u003cp\u003e7 Summary 239\u003c\/p\u003e \u003cp\u003eReferences 240\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 12. Ciprofol (Cipepofol): A γ-Aminobutyric Acid Receptor Agonist for Induction of Anesthesia 251\u003cbr\u003e \u003c\/b\u003e\u003ci\u003eJi Zhang and Dao-Qian Chen\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1 Background 252\u003c\/p\u003e \u003cp\u003e2 Pharmacology 255\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 256\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 261\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 263\u003c\/p\u003e \u003cp\u003e6 Synthesis 264\u003c\/p\u003e \u003cp\u003e7 Summary 268\u003c\/p\u003e \u003cp\u003eReferences 268\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 13. Rimegepant (Nurtec ODT): A CGRP Receptor Antagonist as a Treatment of Episodic Migraine 275\u003cbr\u003e \u003c\/b\u003e\u003ci\u003eYuqi Lavender Zha and Guanglin Luo\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1 Background 276\u003c\/p\u003e \u003cp\u003e2 Pharmacology 278\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 281\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 287\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 287\u003c\/p\u003e \u003cp\u003e6 Synthesis 289\u003c\/p\u003e \u003cp\u003e7 Summary 293\u003c\/p\u003e \u003cp\u003eReferences 293\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 14. Daridorexant (Quviviq): An Antagonist of Orexin Receptors for Treating Insomnia 299\u003cbr\u003e \u003c\/b\u003e\u003ci\u003eDexi Yang\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1 Background 299\u003c\/p\u003e \u003cp\u003e2 Pharmacology 304\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 305\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 311\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 312\u003c\/p\u003e \u003cp\u003e6 Synthesis 314\u003c\/p\u003e \u003cp\u003e7 Summary 318\u003c\/p\u003e \u003cp\u003eReferences 318\u003c\/p\u003e \u003cp\u003e\u003cb\u003eSection IV. Anti-inflammatory Drugs 323\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 15. Deucravacitinib (Sotyktu): A First-in-Class Deuterated TYK2 Inhibitor for the Treatment of Plaque Psoriasis 325\u003cbr\u003e \u003c\/b\u003e\u003ci\u003eDaljit Matharu\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1 Background 325\u003c\/p\u003e \u003cp\u003e2 Pharmacology 330\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 331\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 341\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 342\u003c\/p\u003e \u003cp\u003e6 Synthesis 34 4\u003c\/p\u003e \u003cp\u003e7 Summary 356\u003c\/p\u003e \u003cp\u003eReferences 357\u003c\/p\u003e \u003cp\u003e\u003cb\u003eSection V. Miscellaneous Drugs 361\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 16. Bremelanotide (Vyleesi): A Melanocortin Receptor Agonist for Treating Female Hypoactive Sexual Desire Disorder 363\u003c\/b\u003e\u003cbr\u003e \u003ci\u003eYan Wang\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1 Background 363\u003c\/p\u003e \u003cp\u003e2 Pharmacology 366\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 369\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 370\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 371\u003c\/p\u003e \u003cp\u003e6 Synthesis 372\u003c\/p\u003e \u003cp\u003e7 Summary 377\u003c\/p\u003e \u003cp\u003eReferences 377\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 17. Odevixibat (Bylvay): A Selective Inhibitor of the Ileal Bile Acid Transporter 381\u003cbr\u003e \u003c\/b\u003e\u003ci\u003eAndrew Outlaw and Timothy A. Cernak\u003c\/i\u003e\u003c\/p\u003e \u003cp\u003e1 Background 382\u003c\/p\u003e \u003cp\u003e2 Pharmacology 384\u003c\/p\u003e \u003cp\u003e3 Early Inhibitors of the Ileal Bile Acid Transporter 388\u003c\/p\u003e \u003cp\u003e4 Structure–Activity Relationship (SAR) 388\u003c\/p\u003e \u003cp\u003e5 Pharmacokinetics and Drug Metabolism 393\u003c\/p\u003e \u003cp\u003e6 Efficacy and Safety 393\u003c\/p\u003e \u003cp\u003e7 Synthesis 394\u003c\/p\u003e \u003cp\u003e8 Summary 397\u003c\/p\u003e \u003cp\u003eReferences 398\u003c\/p\u003e \u003cp\u003eIndex 403\u003c\/p\u003e\u003c\/font\u003e\u003c\/p\u003e\r\n\r\n\u003cp\u003e\u003cfont size=\"3\"\u003eSubject Areas: Chemistry [\u003ca title=\"See our other books on Chemistry\" href=\"https:\/\/freshlyprintedbooks.co.uk\/search?q=%22Chemistry%20%5BPN%5D%22\"\u003ePN\u003c\/a\u003e]\u003c\/font\u003e\u003c\/p\u003e\r\n\r\n\r\n\u003c\/font\u003e","brand":"Wiley","offers":[{"title":"Brand New","offer_id":52173688537368,"sku":"9781394225125","price":108.99,"currency_code":"GBP","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0730\/2037\/5320\/files\/9781394225125.jpg?v=1781167129","url":"https:\/\/freshlyprintedbooks.co.uk\/products\/chemistry-and-pharmacology-of-drug-discovery-hardback-9781394225125","provider":"Freshly Printed Books","version":"1.0","type":"link"}