2019 Small Molecule Drug Approvals
2019 was another big year for drug discovery, with 29 FDA novel drug approvals for small molecules (including istradefylline which was first approved in Japan, but not including brilliant blue G, fluorodopa F18, Ga-68-DOTATOC, bremelanotide, afamelanotide, and ferric maltol, which could all be considered small molecules by some definitions) and 3 for antibody-drug-conjugates so far. The ADC approvals include the anti-CD79b agent polatuzumab vedotin (Polivy), the anti-nectin-4 agent enfortumab vedotin (Padcev), and the anti-HER2 agent fam-trastuzumab deruxtecan (Enhertu), all for oncology.
Here is a visual summary of the small molecules with their mechanism of action, indication, and dosing regimen listed (from respective FDA drug labels).
Note: Istradefylline (Nourianz) not included since it was approved in Japan in 2013.
List of 2019 Small Molecule Drug Approvals
List of 2019 Approvals in Oncology (8)
Alpelisib (Piqray) - PI3Kα-sel. inhibitor
Erdafitinib (Balversa) – panFGFR inhibitor
Darolutamide (Nubeqa) – AR antagonist
Fedratinib (Inrebic – JAK2-selective inhibitor
Selinexor (Xpovio) – XPO1 inhibitor
Entrectinib (Rozlytrek) – ROS1/TRK/ALK inhibitor
Zanubrutinib (Brukinsa) – BTK-selective inhibitor
Pexidartinib (Turalio) – CSF1R inhibitor
List of 2019 Approvals in Neurology (9)
Lasmiditan (Reyvow) – 5-HT11F -selective agonist
Ubrogepant (Ulbrelvy) – CGRP receptor antagonist
Lumateperone (Caplyta) – D2/5 – HT2A antagonist
Pitolisant (Wakix) – H3-selective antagonist/inverse agonist
Brexanolone (Zulresso) – GABA AR positive modulator
Cenobamate (Xcopri) – unclear/GABAA-modulator
Siponimod (Mayzent) – S1PR1/5 modulator
Solriamfetol (Sunosi) – dopamine/norepinephrine reuptake inhibitor
Lemborexant (Dayvigo) – OX1R/OX2R dual antagonist
List of 2019 Approvals in Infectious Diseases (3) + Other Areas (4)
Lefamulin (Xenleta) – bacterial ribosome 50S inhibitor
Triclabendazole (Egaten) – Fasciola anthelmintic
Tafamidis (Vyndaqel) – specific transthyretin stabilizer
Voxelotor (Oxbryta) – HbS hemoglobin polymerization inhibitor
Pretomanid – mycolic acid biosynthesis inhibitor
Upadacitinib (Rinvoq) – JAK1 -selective inhibitor
Trifarotene (Aklief) – RARy-selective agonist
Explore drughunter.com for more.
