{"product_id":"current-drug-synthesis-isbn-9781119847250","title":"Current Drug Synthesis","description":"\u003cb\u003eCurrent Drug Synthesis\u003c\/b\u003e \u003cp\u003e\u003cb\u003eThe latest entry in the widely read \u003ci\u003eDrug Synthesis\u003c\/i\u003e series\u003c\/b\u003e  \u003c\/p\u003e\u003cp\u003eIn \u003ci\u003eCurrent Drug Synthesis\u003c\/i\u003e, accomplished medicinal chemist and researcher Dr. Jie Jack Li and 27 expert coauthors deliver an authoritative and comprehensive discussion of the medicinal chemistry of current drugs, as well as the cutting-edge science involved in their synthesis. The book demystifies the process of modern drug discovery for both industry practitioners and students, while capturing the state-of-the-art techniques used to discover some of the most impactful medicines on the market today. \u003c\/p\u003e\u003cp\u003eCovering six different disease areas – including infectious disease, cancer, cardiovascular and metabolic disease, the central nervous system, anti-inflammatory disease, and a miscellaneous section – the book explores 18 different drugs before concluding with chapters on computational drug discovery and peptide drugs.  \u003c\/p\u003e\u003cp\u003eEach chapter includes coverage of background material on a relevant drug class or disease indication and key aspects of drug discovery, including structure-activity relationships, pharmacokinetics, drug metabolism, efficacy, and safety.  \u003c\/p\u003e\u003cp\u003eReaders will also find: \u003c\/p\u003e\u003cul\u003e\n\u003cli\u003eThorough introductions to drugs for infectious diseases, including relebactam, vaborbactam, and baloxavir marboxil\u003c\/li\u003e  \u003cli\u003eIn-depth treatments of cancer-treating drugs, including darolutamide, venetoclax, and osimertinib \u003c\/li\u003e \u003cli\u003eComprehensive explorations of central nervous system drugs, including zuranolone and risdiplam \u003c\/li\u003e \u003cli\u003eExtensive discussions of computational drug discovery and peptide drugs\u003c\/li\u003e\n\u003c\/ul\u003e \u003cp\u003ePerfect for medicinal, organic, synthetic, and process chemists, \u003ci\u003eCurrent Drug Synthesis\u003c\/i\u003e will also earn a place in the libraries of research scientists working in lead optimization and process development, as well as graduate students studying organic chemistry, heterocyclic chemistry, or medicinal chemistry.  Preface xi \u003c\/p\u003e\u003cp\u003eContributing Authors xiii\u003c\/p\u003e \u003cp\u003e\u003cb\u003ePart I Infectious Disease Drugs 1 \u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 1 Relebactam (Recarbrio), A β-Lactamase Inhibitor for the Treatment of cIAI\/cUTI\/HABP\/ VABP 3\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e1 Background 3\u003c\/p\u003e \u003cp\u003e2 Pharmacology 5\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 6\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 9\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 10\u003c\/p\u003e \u003cp\u003e6 Syntheses 10\u003c\/p\u003e \u003cp\u003e7 Summary 14\u003c\/p\u003e \u003cp\u003e8 References 14\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 2 Vaborbactam (in Combination with Meropenem as Vabomere), a Non-β-Lactam β-Lactamase Inhibitor for Treatment of Complicated Urinary Tract Infections and Pyelonephritis \u003c\/b\u003e\u003cb\u003e17\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e1 Background 17\u003c\/p\u003e \u003cp\u003e2 Discovery Medicinal Chemistry 21\u003c\/p\u003e \u003cp\u003e3 Vaborbactam\/Vabomere Clinical Trials 27\u003c\/p\u003e \u003cp\u003e4 Vaborbactam Medicinal Chemistry Synthesis 29\u003c\/p\u003e \u003cp\u003e5 Vaborbactam Process Chemistry Synthesis 30\u003c\/p\u003e \u003cp\u003e6 Conclusions 37\u003c\/p\u003e \u003cp\u003e7 References 38\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 3 Baloxavir Marboxil (Xofluza), A Cap-Dependent Endonuclease Inhibitor for Treating Influenza 41 \u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e1 Background 41\u003c\/p\u003e \u003cp\u003e2 Mechanism of Action 43\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship 45\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 49\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 50\u003c\/p\u003e \u003cp\u003e6 Syntheses 50\u003c\/p\u003e \u003cp\u003e7 Summary 54\u003c\/p\u003e \u003cp\u003e8 References 54\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 4 Process Chemistry Development of the HIV Protease Inhibitor Drug Kaletra: A Mixture of Ritonavir and Lopinavir 57 \u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e1 Background 58\u003c\/p\u003e \u003cp\u003e2 Ritonavir Portion of Kaletra Synthesis 58\u003c\/p\u003e \u003cp\u003e3 Discovery Synthesis of the Ritonavir Core 60\u003c\/p\u003e \u003cp\u003e4 Discovery Synthesis of Ritonavir Wing Pieces 63  \u003c\/p\u003e \u003cp\u003e5 Large-Scale Process Chemistry Synthesis of the  Ritonavir Core 65\u003c\/p\u003e \u003cp\u003e6 Large-Scale Syntheses of the 5-Hydroxymethyl  Thiazole Wing Portion 69\u003c\/p\u003e \u003cp\u003e7 The Large-Scale Coupling of the Thiazole  Wing Pieces to the Core 70\u003c\/p\u003e \u003cp\u003e8 Lopinavir Portion of Kaletra—  Discovery Synthesis and Process Development 72\u003c\/p\u003e \u003cp\u003e9 Discovery Synthesis of Lopinavir 73\u003c\/p\u003e \u003cp\u003e10 Discovery Synthesis of Wing Pieces 74\u003c\/p\u003e \u003cp\u003e11 Process Improvements to the Wing Pieces 76\u003c\/p\u003e \u003cp\u003e12 Optimization of Lopinavir Synthesis with Intermediates 78\u003c\/p\u003e \u003cp\u003e13 Conclusions 81\u003c\/p\u003e \u003cp\u003e14 References 81\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 5 Eravacycline (Xerava), A Novel and Completely Synthetic Fluorocycline Antibiotic 85 \u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e1 Background 85\u003c\/p\u003e \u003cp\u003e2 Pharmacology 89\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 91\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 93\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 93\u003c\/p\u003e \u003cp\u003e6 Syntheses 93\u003c\/p\u003e \u003cp\u003e7 Summary 98\u003c\/p\u003e \u003cp\u003e8 References 99\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 6 Albuvirtide (Aikening), A gp41 Analog as an HIV-1 Fusion Inhibitor 101 \u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e1 Background 101\u003c\/p\u003e \u003cp\u003e2 Pharmacology 102\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 106\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 107\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 110\u003c\/p\u003e \u003cp\u003e6 Syntheses 112\u003c\/p\u003e \u003cp\u003e7 Summary 114\u003c\/p\u003e \u003cp\u003e8 References 115\u003c\/p\u003e \u003cp\u003e\u003cb\u003ePart II Cancer Drugs 119 \u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 7 Darolutamide (Nubeqa): An Androgen Receptor  Antagonist for Treating Nonmetastatic, Castration-Resistant 121 \u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e1 Background 121\u003c\/p\u003e \u003cp\u003e2 Pharmacology 124\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 126\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 132\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 134\u003c\/p\u003e \u003cp\u003e6 Syntheses 135\u003c\/p\u003e \u003cp\u003e7 The Future 137\u003c\/p\u003e \u003cp\u003e8 References 138\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 8 Venetoclax (Venclexta): A BCL-2 Antagonist for Treating Chronic Lymphocytic Leukemia 143 \u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e1 Background 143\u003c\/p\u003e \u003cp\u003e2 Pharmacology 144\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 147\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 153\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 154\u003c\/p\u003e \u003cp\u003e6 Syntheses 155\u003c\/p\u003e \u003cp\u003e7 Summary 160\u003c\/p\u003e \u003cp\u003e8 References 161\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 9 Osimertinib (Tagrisso), A Potent and Selective Third-Generation EGFR Inhibitor for the Treatment of Both Sensitizing and T790M-Resistance Mutations 165 \u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e1 Background 165\u003c\/p\u003e \u003cp\u003e2 Pharmacology 167\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 170\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 173\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 174\u003c\/p\u003e \u003cp\u003e6 Syntheses 175\u003c\/p\u003e \u003cp\u003e7 Summary 180\u003c\/p\u003e \u003cp\u003e8 References 180\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 10 Sotorasib (LUMAKRA), An Irreversible Covalent Inhibitor of KRASG12C 183 \u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e1 Background 183\u003c\/p\u003e \u003cp\u003e2 Pharmacology 184\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 186\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 191\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 191\u003c\/p\u003e \u003cp\u003e6 Syntheses 192\u003c\/p\u003e \u003cp\u003e7 Summary 196\u003c\/p\u003e \u003cp\u003e8 References 196\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 11 Lorlatinib (Lorbrena), An ALK Inhibitor for Treating NSCLC 201 \u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e1 Background 201\u003c\/p\u003e \u003cp\u003e2 Pharmacology 203\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 205\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 210\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 211\u003c\/p\u003e \u003cp\u003e6 Syntheses 213\u003c\/p\u003e \u003cp\u003e7 Summary 226\u003c\/p\u003e \u003cp\u003e8 References 227\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 12 Niraparib (Zejula) A Small Molecule, PARP1\/2 Inhibitor for Treating Breast, Ovarian, and Pancreatic Cancers 231\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e2 Pharmacology 235\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 238\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 243\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 243\u003c\/p\u003e \u003cp\u003e6 Syntheses 244\u003c\/p\u003e \u003cp\u003e7 Summary 248\u003c\/p\u003e \u003cp\u003e8 References 248\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 13 Selinexor (Xpovio), An XPO1 Inhibitor and a New Class of Therapeutics for Treating Multiple Myeloma 253\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e1 Exportin1 (XPO1) 253\u003c\/p\u003e \u003cp\u003e2 Overview of Multiple Myeloma 255\u003c\/p\u003e \u003cp\u003e3 Development of Selinexor 256\u003c\/p\u003e \u003cp\u003e4 Pharmacology and Mechanism 257\u003c\/p\u003e \u003cp\u003e5 Pharmacokinetics, Pharmacodynamics and Drug Metabolism 258\u003c\/p\u003e \u003cp\u003e6 Efficacy and Safety 259\u003c\/p\u003e \u003cp\u003e7 Syntheses 259\u003c\/p\u003e \u003cp\u003e8 Summary and Future 262\u003c\/p\u003e \u003cp\u003e9 References 262\u003c\/p\u003e \u003cp\u003e\u003cb\u003ePart III Cns Drugs 265\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 14 Sage 217 (Zuranolone) for Treating Major of Depressive Disorder267\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e1 Background 267\u003c\/p\u003e \u003cp\u003e2 Pharmacology 270\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 272\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 279\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 280\u003c\/p\u003e \u003cp\u003e6 Syntheses 281\u003c\/p\u003e \u003cp\u003e7 Summary 282\u003c\/p\u003e \u003cp\u003e8 References 283\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 15 Risdiplam (Evrysdi), A Small Molecule, SMN2-directed RNA Splicing Modifier for Treating Spinal Muscular Atrophy 287\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e1 Background 287\u003c\/p\u003e \u003cp\u003e2 Pharmacology 289\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 290\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 297\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 297\u003c\/p\u003e \u003cp\u003e6 Syntheses 298\u003c\/p\u003e \u003cp\u003e7 Summary 300\u003c\/p\u003e \u003cp\u003e8 References 301\u003c\/p\u003e \u003cp\u003e\u003cb\u003ePart IV Miscellaneous Drugs 305\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 16 Esaxerenone (Minnebro), An Oral, Non-steroidal, Selective Mineralocorticoid Receptor Blocker for the Treatment of Essential Hypertension307\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e1 Background 307\u003c\/p\u003e \u003cp\u003e2 Pharmacology 310\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 311\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 313\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 315\u003c\/p\u003e \u003cp\u003e6 Syntheses 316\u003c\/p\u003e \u003cp\u003e7 Summary 320\u003c\/p\u003e \u003cp\u003e8 References 321\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 17 Voclosporin (Lupkynis), A Macrocyclic Peptide Inhibitor of Calcineurin for the Treatment of Lupus Nephritis 323\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e1 Background 323\u003c\/p\u003e \u003cp\u003e2 Pharmacology 326\u003c\/p\u003e \u003cp\u003e3 Structure–Activity Relationship (SAR) 326\u003c\/p\u003e \u003cp\u003e4 Pharmacokinetics and Drug Metabolism 329\u003c\/p\u003e \u003cp\u003e5 Efficacy and Safety 331\u003c\/p\u003e \u003cp\u003e6 Syntheses 333\u003c\/p\u003e \u003cp\u003e7 References 336\u003c\/p\u003e \u003cp\u003e\u003cb\u003eChapter 18 Computational-Aided Drug Design 339\u003c\/b\u003e\u003c\/p\u003e \u003cp\u003e1 Background 339\u003c\/p\u003e \u003cp\u003e2 Structure-based Drug Design (SBDD) 341\u003c\/p\u003e \u003cp\u003e3 Ligand-based Drug Design (LBDD) 352\u003c\/p\u003e \u003cp\u003e4 Summary 361\u003c\/p\u003e \u003cp\u003e5 References 362\u003c\/p\u003e \u003cp\u003eIndex 373\u003c\/p\u003e  \u003cp\u003e\u003cb\u003eJie Jack Li, PhD,\u003c\/b\u003e is the CSO of GenHouse Bio. Previously, he was VP of Discovery Chemistry at ChemPartner, an Associate Professor of Chemistry at the University of San Francisco and a Medicinal Chemist at Pfizer and Bristol-Myers Squibb. He has authored or edited over 30 books, including \u003ci\u003eMedicinal Chemistry for Practitioners\u003c\/i\u003e published by Wiley in 2020.   \u003c\/p\u003e\u003cp\u003e\u003cb\u003eThe latest entry in the widely read \u003ci\u003eDrug Synthesis\u003c\/i\u003e series\u003c\/b\u003e  \u003c\/p\u003e\u003cp\u003eIn \u003ci\u003eCurrent Drug Synthesis\u003c\/i\u003e, accomplished medicinal chemist and researcher Dr. Jie Jack Li and 27 expert coauthors deliver an authoritative and comprehensive discussion of the medicinal chemistry of current drugs, as well as the cutting-edge science involved in their synthesis. The book demystifies the process of modern drug discovery for both industry practitioners and students, while capturing the state-of-the-art techniques used to discover some of the most impactful medicines on the market today. \u003c\/p\u003e\u003cp\u003eCovering six different disease areas – including infectious disease, cancer, cardiovascular and metabolic disease, the central nervous system, anti-inflammatory disease, and a miscellaneous section – the book explores 18 different drugs before concluding with chapters on computational drug discovery and peptide drugs.  \u003c\/p\u003e\u003cp\u003eEach chapter includes coverage of background material on a relevant drug class or disease indication and key aspects of drug discovery, including structure-activity relationships, pharmacokinetics, drug metabolism, efficacy, and safety.  \u003c\/p\u003e\u003cp\u003eReaders will also find: \u003c\/p\u003e\u003cul\u003e\n\u003cli\u003eThorough introductions to drugs for infectious diseases, including relebactam, vaborbactam, and baloxavir marboxil\u003c\/li\u003e  \u003cli\u003eIn-depth treatments of cancer-treating drugs, including darolutamide, venetoclax, and osimertinib \u003c\/li\u003e \u003cli\u003eComprehensive explorations of central nervous system drugs, including zuranolone and risdiplam \u003c\/li\u003e \u003cli\u003eExtensive discussions of computational drug discovery and peptide drugs\u003c\/li\u003e\n\u003c\/ul\u003e \u003cp\u003ePerfect for medicinal, organic, synthetic, and process chemists, \u003ci\u003eCurrent Drug Synthesis\u003c\/i\u003e will also earn a place in the libraries of research scientists working in lead optimization and process development, as well as graduate students studying organic chemistry, heterocyclic chemistry, or medicinal chemistry.\u003c\/p\u003e","brand":"Wiley","offers":[{"title":"Default Title","offer_id":47989015544037,"sku":"NP9781119847250","price":195.0,"currency_code":"USD","in_stock":false}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/1842\/7735\/files\/9781119847250.jpg?v=1761782443","url":"https:\/\/k12savings.com\/products\/current-drug-synthesis-isbn-9781119847250","provider":"K12savings","version":"1.0","type":"link"}