2021 Small Molecule Drug Approvals Review
We’ll be reviewing 2021’s novel FDA drug approvals in a series of articles, starting with this high-level overview of the small molecule drugs approved by the FDA in 2021. You can find Part 2 on First-in-Class Small Molecules here and the 2021 Large Molecules series here. Our deep dive on Small Molecule Oncology Approvals is also live.
together with Jen Huen, Vinicius Texeira, Naveed Yasin, Maria Koyioni, and Adrian Parodi
There were:
50 novel drugs approved in 2021
32 small molecules in this group (including peptides, excluding radiologics)
16 large molecules
27 “first-in-class” drugs
For small molecules, there were:
9 in oncology
5 in neurology
5 for genetic conditions
4 for infectious diseases
3 in immunology
2 in endocrinology
1 in dermatology
1 in hematology
1 in cardiology
1 in family medicine
Three of our favorite molecules are shown below:
Our complete, hi-res compilation of all 32 of the small molecule drugs with structures, drug targets and mechanisms of action, doses and routes of administration, and indication appears below. You can find past examples of our 2020 Small Molecule Approvals Poster and 2019 Small Molecule Approvals Poster online.
List of 2021 Novel Small Molecule Drug Approvals
Highlights from 2021 Small Molecule Approvals
Ibrexafungerp (Brexafemme) – β-1,3-glucan synthesis inhibitor
Atogepant (Qulipta) – calcitonin gene-related peptide
Sotorasib (Lumakras) – KRASG12C GTPase inhibitor
List of Novel 2021 Small Molecule Drug Approvals in Oncology (9)
Umbralisib (Ukoniq) – PI3Kδ and CK1ε kinase inhibitor
Melphalan flufenamide (Pepaxto*) – peptide-conjugated alkylating agent, withdrawn
Sotorasib (Lumakras) – KRASG12C GTPase inhibitor
Infigratinib (Truseltiq) – pan-FGFR kinase inhibitor
Tepotinib (Tepmetko) – MET kinase inhibitor
Tivozanib (Fotivda) – pan-VEGFR kinase inhibitor
mobocertinib (Exkinity) – EGFR exon 20 insertion kinase
Trilaciclib (Cosela) – CDK4 and 6 kinase inhibitor
asciminib (Scemblix) – ABL/BCR-ABL1 kinase allosteric inhibitor
List of Novel 2021 Small Molecule Drug Approvals in Neurology (5)
samidorphan + olanzapine (Lybalvi) – opioid antagonist
atogepant (Qulipta) – calcitonin gene-related peptide antagonist
ponesimod (Ponvory) – sphingosine 1-phosphate (S1P) modulator
viloxazine (Qelbree) – selective norepinephrine reuptake inhibitor
serdexmethylphenidate + dexmethylphenidate (Azstarys) – catecholamine reuptake inhibitor
List of Novel 2021 Small Molecule Drug Approvals for Genetic Conditions (5)
maralixibat (Livmarli) – ileal bile acid transporter
belzutifan (Welireg) – hypoxia-inducible factor 2α
odevixibat (Bylvay) – ileal bile acid transporter
fosdenopterin (Nulibry) – cyclic pyranopterin monophosphate (cPMP)
vosoritide (Voxzogo) – C-type natriuretic peptide analog
List of Novel 2021 Small Molecule Drug Approvals for Infectious Diseases (4)
cabotegravir + rilpivirine (Cabenuva) – HIV1 integrase strand transfer
maribavir (Livtencity) – CMV pUL97 kinase inhibitor
(Brexafemme) – β-1,3-glucan sysnthesis inhibitor
fexinidazole (Fexinidazole) – nitroimidazole antimicrobial
List of Novel 2021 Small Molecule Drug Approvals in Endocrinology (2)
finerenone (Kerendia) – non-steroidal mineralocorticoid
dasiglucagon (Zegalogue) – antihypoglycemic, glucagon
List of Novel 2021 Small Molecule Drug Approvals in Immunology (3)
voclosporin (Lupkynis) – calcineurin inhibitor
avacopan (Tavneos) – complement C5a receptor antagonist
belumosudil (Rezurock) – selective ROCK2 kinase inhibitor
Other Areas (4)
difelikefalin (Korsuva) – kappa opioid receptor agonist
vericiguat (Verquvo) – guanylate cyclase stimulator
pegcetacoplan (Empaveli) – complement C3 inhibitor
estetrol + drospirenone (Nextstellis) – naturally-occurring estrogen E4
Found this helpful? Explore drughunter.com for more drug discovery resources that help you save time, stay up-to-date, and discover ideas.
You can find Part 2 on First-in-Class Small Molecules here and the 2021 Large Molecules series here. Our deep dive on Small Molecule Oncology Approvals is also live.