54 small molecule drugs containing a pyridine ring approved by the FDA

Heterocyclic skeletons, especially pyridine-containing nitrogen heterocycles, have been the main components of drugs approved over the past decade. Between 2014 and 2023, the U.S. Food and Drug Administration (FDA) approved 54 small molecule drugs containing pyridine rings.

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In the article “The 35 Most Common Nitrogen Heterocyclic Structures in Drugs,” pyridine is the most frequently occurring nitrogen-containing heterocycle, ranking first.

The largest number of these drugs are anticancer drugs (18, accounting for 33%), followed by drugs affecting the central nervous system (CNS) (11, accounting for 20%). These include drugs used to treat migraines, Parkinson’s disease, chemotherapy-induced nausea, insomnia, attention deficit hyperactivity disorder (ADHD), or analgesics or sedatives with central nervous system effects. Next, 6 drugs (11%) are approved for the treatment of rare diseases, followed by 5 drugs affecting the hematopoietic system.

The following section introduces marketed drug molecules containing a pyridine ring:

Abemaciclib (brand name: Verzenio) is indicated for breast cancer and was approved for marketing in 2017.

Palbociclib (brand name: Ibrance) is indicated for breast cancer and was approved for marketing in 2015.

Ribociclib (trade name: Kisqali) is indicated for gastrointestinal stromal tumors and was approved for marketing in 2017.

Trilaciclib (brand name: Cosela) is indicated for myeloprotection and was approved for marketing in 2021.

Acalabrutinib (trade name: Calquence) is indicated for non-Hodgkin’s lymphoma and was approved for marketing in 2017.

Asciminib (brand name: Scemblix) is indicated for chronic myeloid leukemia and was approved for marketing in 2021.

Neratinib (brand name: Nerlynx) is indicated for breast cancer and was approved for marketing in 2017.

Pexidartinib (trade name: Turalio) is indicated for giant cell tumor of the tendon sheath and was approved for marketing in 2019.

Pralsetinib (brand name: Gavreto) is indicated for thyroid cancer and was approved for marketing in 2020.

Selpercatinib (trade name: Retevmo) is indicated for solid tumors and was approved for marketing in 2020.

Ripretinib (brand name: Qinlock) is indicated for gastrointestinal stromal tumors and was approved for marketing in 2020.

Alpelisib (brand name: Piqray) is indicated for breast cancer and was approved for marketing in 2019.

Lorlatinib (trade name: Lorbrena) is indicated for non-small cell lung cancer and was approved for marketing in 2018.

Apalutamide (brand name: Erleada) is indicated for prostate cancer and was approved for marketing in 2018.

Enasidenib (brand name: Idhifa) is indicated for acute myeloid leukemia and was approved for marketing in 2017.

Ivosidenib (brand name: Tibsovo) is indicated for acute myeloid leukemia and was approved for marketing in 2018.

Sonidegib (brand name: Odomzo) is indicated for skin cancer and was approved for marketing in 2015.

Sotorasib (brand name: Lumakras) is indicated for lung cancer and was approved for marketing in 2021.

Abametapir (brand name: Xeglyze) is indicated for head lice and was approved for marketing in 2020.

Amifampridine, brand names: Firdapse, Ruzurgi, is indicated for Lambert-Eton myasthenic syndrome (LEMS) and was approved for marketing in 2018.

Atogepant (brand name: Qulipta) is indicated for migraines and was approved for marketing in 2021.

Rimegepant (brand name: Nurtec) is indicated for migraines and was approved for marketing in 2020.

Ubrogepant, brand name Upelvy, is indicated for migraines and was approved for marketing in 2019.

Lasmiditan (brand name: Reyvow) is indicated for migraine and was approved for marketing in 2019.

Betrixaban (brand name: BEVYXXA) is indicated for anticoagulation and was approved for marketing in 2017.

Edoxaban, brand names: Lixiana, Savaysa, is indicated for anticoagulation and was approved for marketing in 2015.

Avatrombopag (brand name: Doptelet) is indicated for liver disease-related thrombocytopenia and was approved for marketing in 2018.

Delafloxacin (trade name: Baxdela) is an antibiotic approved for marketing in 2017.

Finerenone (brand name: Kerendia) is indicated for kidney disease and was approved for marketing in 2021.

Ozenoxacin (brand name: Ozanex) is indicated for impetigo and was approved for marketing in 2017.

Tedizolid phosphate (brand name: Sivextro) is indicated for acute bacterial skin and soft tissue infections caused by susceptible bacteria in adults. It was approved for marketing in 2014.

Elexacaftor (trade name: Trikafta) is indicated for cystic fibrosis and was approved for marketing in 2019.

Lumacaftor (trade name: Orkambi) is indicated for cystic fibrosis and was approved for marketing in 2015.

Fostamatinib (brand name: Tavalisse) is indicated for chronic immune thrombocytopenic purpura (ITP) and was approved for marketing in 2018.

Fosnetupitant (brand name: Akynzeo) is indicated for nausea and vomiting caused by chemotherapy and was approved for marketing in 2018.

Netupitant (brand name: Akynzeo) is indicated for nausea and vomiting caused by chemotherapy and was approved for marketing in 2014.

Isavuconazonium (trade name: Cresemba) is indicated for antifungal purposes and was approved for marketing in 2015.

Oteseconazole (trade name: Vivjoa) is indicated for recurrent vulvovaginal candidiasis (RVVC) and was approved for marketing in 2022.

Lonafarnib, brand name Zokinvy, is indicated for Hutchinson-Gilford progeria syndrome (HGPS) and was approved for marketing in 2020.

Litostat (Leniolisib), brand name: Joenja, is indicated for activated phosphoinositol 3-kinase delta syndrome (APDS) and was approved for marketing in 2023.

Orlieridine (brand name: Olinvyk) is indicated as an analgesic and was approved for marketing in 2022.

Lemborexant, brand name Dayvigo, is indicated for insomnia and was approved for marketing in 2019.

Omidenepag (brand name: Omlonti) is indicated for glaucoma and was approved for marketing in 2022.

Opicapon (brand name: Ongentys) is indicated for Parkinson’s disease and was approved for marketing in 2020.

Lenapavir, with no brand name, is indicated for HIV-AIDS and was approved for marketing in 2022.

Remimazolam (brand name: Byfavo) is indicated as a sedative and was approved for marketing in 2020.

Serdex methylphenidate, brand name Azstarys, is indicated for attention deficit hyperactivity disorder (ADHD) and was approved for marketing in 2021.

Tirbanibulin (trade name: Kilsyr) is indicated for actinic keratosis and was approved for marketing in 2020.

Vonoprazan (brand name: Voquezna) is indicated for gastric ulcers and was approved for marketing in 2022.

Voxelotor (brand name: Oxbryta) is indicated for sickle cell disease and was approved for marketing in 2019.

Vorapaxar, brand name Zontivity, is indicated for antiplatelet therapy and was approved for marketing in 2014.

Flutaucipir-F18, with no brand name, is indicated for Alzheimer’s disease (AD) and was approved for marketing in 2020.

Piflufolastat F-18, marketed as Pylarify, is indicated for prostate cancer and was approved for marketing in 2021.

Gadopiclenol (trade name: Elucirem) is indicated for the visualization and detection of lesions and abnormal blood vessels and was approved for marketing in 2022.