2020 Small Molecule Drug Approvals
On Jun. 23rd at 11AM PST, Dewakar Sangaraju and Dennis Hu gave a PBSS/CLSA webinar titled “Highlights from 2020’s FDA New Drug Approvals,” organized by Cyrus Khojasteh and Shichang Miao. One interesting fact about each approved small molecule drug was shared, along with statistics and specific case studies from the cohort of interest to the audience.
Subscribers can get a complete visual list with the structures of 2020 FDA new drug approvals by contacting info@drughunter.com. 2020’s large molecule FDA new drug approvals can be found here. The list of 2020 FDA approved drugs also contains drug route of administration, mechanism of action, dosing, main trial outcome or primary endpoint, NCT trial #’s for pivotal trials (Ph. III unless otherwise specified), number of patients enrolled in the pivotal trials at the time of approval, specialty and indication, all summarized from the FDA drug labels or clinical trial entries linked below. There is no meaning to the order in which drugs are presented.
Disclaimer: This information is shared for educational purposes only, is intended for research professionals, is not medical advice, is not shared on behalf of any of the contributors’ employers, and is not an endorsement of any of these products. Complete safety information can be found in each drug’s FDA label.
List of 2020 Small Molecule Drug Approvals
Zeposia (ozanimod) – oral S1P(1/5) receptor modulator – NCT02294058; NCT02047734
Nurtec ODT (rimegepant) – oral CGRP GPCR antagonist – NCT03461757
Tazverik (tazemetostat – oral EZH2 methyltransferase inhibitor – NCT02601950
Retevmo (selpercatinib) – oral RET fusion kinase inhibitor (WT+mut) – NCT03157128
Rukobia (fostemsavir) – oral HIV-1 gp120 attachment inhibitor – NCT02362503
Veklury (remdesivir) – IV nucleotide RNA polymerase inhibitor – NCT04280705; NCT04292899; NCT04292730
Orladeyo (berotralstat) – oral plasma kallikrein inhibitor – NCT3485911
Inqovi (decitabine and cedazuridine) – oral nucleoside cytidine deaminase inhibitor – NCT02103478 ; NCT03306264
Gemtesa (vibegron) – oral selective β3 adrenergic receptor agonist – NCT03492281
Zokinvy (lonafarnib)- oral farnesyltransferase inhibitor – NCT00425607 ; NCT00916747
Ongentys (opicapone)- oral COMT enzyme inhibitor – NCT01568073; NCT01227655
Koselugo (selumetinib) – oral MEK1/2 kinase inhibitor – NCT01362803
Zepzelca (lurbinectedin) – IV DNA alkyating agent – NCT02454972
Orgovyx (relugolix) – oral GnRH hormone receptor antagonist – NCT03085095
Evrysdi (risdiplam)- oral SMN RNA splicing modifier – NCT02913482; NCT02908685
Byfavo (remimazolam) – IV GABAA receptor modulator – NCT02290873; NCT02296892; NCT02532647
Olinvyk (oliceridine) – IV opioid receptor agonist – NCT02820324
Ayvakit (avapritinib) – oral PDGFRA + KIT kinase inhibitor – NCT02508532
Tabrecta (capmatinib) – oral MET kinase inhibitor – NCT02414139
Gavreto (pralsetinib) – oral RET fusion kinase inhibitor (WT+mut) – NCT03037385
Pemazyre (pemigatinib) – oral FGFR1/2/3 kinase inhibitor – NCT02924376
Qinlock (ripretinib) – oral KIT + PDGFRA kinase inhibitor – NCT03353753
Tukysa (tucatinib) – oral HER2 kinase inhibitor – NCT02614794
Isturisa (osilodrostat) – oral cortisol synthesis inhibitor – NCT02180217
Winlevi (clascoterone) – topical androgen receptor inhibitor – NCT02608450; NCT02608476
Klisyri (tirbanibulin) – topical microtubule inhibitor – NCT03285477; NCT03285490
Nexletol (bempedoic acid) – oral ATP citrate synthase enzyme inhibitor – NCT02666664; NCT02991118
Xeglyze (abametapir) – topical metalloproteinase inhibitor – NCT02060903 ; NCT02062060
Tauvid (flortaucipir F18) – IV tau protein aggregate radiodiagnostic – NCT02516046; NCT03901092
Detectnet (copper Cu 64 dotatate injection) – IV somatostatin rcpt. (SSTR2) radiodiagnostic – NCT04334837
Cerianna (fluoroestradiol F18) – IV ER-binding radiodiagnostic – NCT01986569
Gallium 68 (Gallium 68 PSMA-11) – IV PSMA-binding radiodiagnostic – NCT02919111; NCT02918357
Artesunate (artesunate) – IV artemisinin-based antimalarial
Lampit (nifurtimox) – oral antiprotozoal – NCT02625974
Pizensy (lactitol) – oral osmotic laxative – NCT02819297; NCT02481947
Dojolvi (triheptanoin) – oral fatty acid replacement
Imcivree (Setmelanotide) – subcutaneous MC4 receptor agonist – NCT02896192; NCT03287960
Barhemsys (amisulpride) – IV selective dopamine D2/3 receptor antag. – NCT01991860; NCT02337062
List of Novel APIs Among FDA Drug Approvals in 2020 (Formatted Without Links)
ozanimod (Zeposia) – oral S1P1/5 receptor modulator
rimegepant (Nurtec ODT) – oral CGRP GPCR antagonist
tazemetostat (Tazverik) – oral EZH2 methyltransferase inhibitor
selpercatinib (Retevmo) – oral RET fusion kinase inhibitor (WT + mutant)
fostemvasir (Rukobia) – oral HIV-1 gp120 attachment inhibitor
remdesivir (Veklury) – IV nucleotide RNA polymerase inhibitor
berotralstat (Orladeyo) – oral plasma kallikrein inhibitor
cedazuridine (Inqovi) – oral nucleoside cytidine deaminase inhibitor
vibegron (Gemtesa) – oral selective B3 adrenergic receptor agonist
Ionafarnib (Zokinvy) – oral farnesyltransferase inhibitor
opicapone (Ongentys) – oral COMT enzyme inhibitor
selumetinib (Koselgo) – oral MEK1/2 kinase inhibitor
lurbinectedin (Zepelca) – IV DNA alkylating agent
relugolix (Orgovyx) – oral GnRH hormone receptor antagonist
risdiplam (Evrysdi) - oral SMN RNA splicing modifier
remimazolam (Byfavo) - IV GABAA receptor modulator
oliceridine (Olinvyk) - IV opioid receptor agonist
avapritinib (Ayvakit) - oral PDGFRA + KIT kinase inhibitor
capmatinib (Tabrecta) - oral MET kinase inhibitor
pralsetinib (Gavreto) - oral RET fusion kinase inhibitor (WT+mut)
pemigatinib (Pemazyre) - oral FGFR1/2/3 kinase inhibitor
ripretinib (Qinlock) - oral KIT + PDGFRA kinase inhibitor
tucatinib (Tukysa) - oral HER2 kinase inhibitor
osildrostat (Isturisa) - oral cortisol synthesis inhibitor
clascoterone (Winlevi) - topical androgen receptor inhibitor
tirbanibulin (Klisyri) - topical microtubule inhibitor
bempedoic acid (Nexletol) - oral ATP citrate synthase enzyme inhibitor
abametapir (Xeglyze) - topical metalloproteinase inhibitor
flortaucipir F18 (Tauvid) - IV tau protein aggregate radiodiagnostic
64Cu dotatate (Detectnet) - IV somatostatin rcpt. (SSTR2) radiodiagnostic
fluoroestradiol 18F (Cerianna) - IV ER-binding radiodiagnostic
68Ga PSMA-11 - IV PSMA-binding radiodiagnostic
artesunate (Artesunate) - IV artemisinin-based antimalarial
nifurtimox (Lampit) - oral antiprotozoal
lactitol (Pizensy) - oral osmotic laxative
triheptanoin (Dojolvi) - oral fatty acid replacement
amisulpride (Barhemsys) - IV selective dopamine D2/3 receptor antagonist
setmelanotide (Imcivree) - subcutaneous MC4 receptor agonist
More details will be shared after the webinar on Jun. 23rd. Explore drughunter.com for more drug discovery articles.