2019 was another big year for drug discovery, with 29 FDA novel drug approvals for small molecules1 and 3 for antibody-drug-conjugates so far.2

Here is a visual summary of the small molecules with their mechanism of action, indication, and dosing regimen listed.3 Happy new year, and looking forward to a great 2020! You can find a higher resolution PDF at the bottom of the page.

2019 Small Molecule Drug Approvals
Note: Istradefylline (Nourianz) not included since it was approved in Japan in 2013.

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Oncology:

  1. Alpelisib (Piqray) – PI3Ka-sel. inhibitor – HER2+/HR- BC – oral: 300 mg QD
  2. Erdafitinib (Balversa) – pan-FGFR inhibitor – FGFR+met. Urothelial carcinoma – oral: 8 mg QD
  3. Darolutamide (Nubeqa) – AR antagonist – nmCR prostate cancer – oral: 300 mg BID
  4. Fedratinib (Inrebic) – JAK2-sel. Inhibitor – high risk myelofibrosis – oral: 400 mg QD
  5. Selinexor (Xpovio) –  XPO1 inhibitor – RR-multiple myeloma – oral: 80 mg BIW
  6. Entrectinib (Rozlytrek) – ROS1/TRK/ALK inhibitor – ROS1+/NTRK+ cancers – oral: 600 mg QD
  7. Zanubrutinib (Brukinsa) – BTK-sel.  inhibitor – mantle cell lymphoma – oral: 320 mg QD
  8. Pexidartinib (Turalio) – CSF1R inhibitor – tenosyn/ giant cell tumor – oral: 400 mg BID

Neurological Disorders

  1. Lasmiditan (Reyvow) – 5-HT1F-sel.  Agonist migraine termination oral: 5—200 mg QD
  2. Ubrogepnat (Ulbrelvy) – CGRP receptor antagonist – migraine – oral:50 mg QD
  3. Lumateperone (Caplyta) –  D2/5-HT2A antagonist schizophrenia oral: 42 mg QD
  4. Brezanolone (Zulresso) – GABAAR +ive modulator postpartum depression continuous IV (60 h)
  5. Cenobamate (Xcopri) – unclear/GABAA-mod. Partial-onset seizures – oral: 200 mg QD
  6. Siponimod (Mayzent) – S1PR1/5 modulator – multiple sclerosis – oral: 2 mg QD
  7. Pitolisant (Wakix) – H3-sel. Antagonist/inverse agonist – EDS / narcolepsy – oral: up to 37 mg QD
  8. Solriamfetol (Sunosi) – dopamine/norep. Reuptake inhibitor – EDS / narcolepsy – oral: up to 150 mg QD
  9. Lemborexant (Dayvigo) – OX1R / OX2R – insomnia – oral: up to 10 mg QD

Infectious Diseases

  1. Lefamulin (Xenleta) – bact. Ribosome 50S – bacterial pneumonia – oral: 60 mg BID
  2. Triclabendazole (Egaten) – Fasciola anthelmintic – fascioliasis – oral: 10mg/kg BID
  3. Premotanid – mycolic acid biosynth.  inh. – drug resistant TB – oral: 200 mg QD
  4. Relebactam (Recarbio) – beta-lactamase inhibitor – cUTI + cIAI infections – IV: 250 mg
  5. Cefidericol (Fetroja) – penicillin binding proteins – complated UTI – IV: 2 g TID

Other

  1. Elexacaftor (in Trikafta) – CFTR corrector – cystic fibrosis – oral: 200 mg QD
  2. Upadacitinib (Rinvoq) – JAK1-sel.  Inhibitor – moderate/severe RA oral: 15 mg QD
  3. Voxelotor (Oxbryta) – HbS polymerization inhibitor – sickle cell disease – oral:  1500 mg QD
  4. Tenapanor (Ibsrela) – NHE3 inhibitor – IBS-C – gut-restricted, 50 mg BID
  5. Tafamidis (Vyndaqel) – specific transthyretin stabilizer – cardiomyopathy – oral: 80 mg QD

Explore drughunter.com for more.

  1. 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: https://www.fda.gov/drugs/new-drugs-fda-cders-new-molecular-entities-and-new-therapeutic-biological-products/novel-drug-approvals-2019
  2. 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.
  3. From respective FDA drug labels.