2022, FDA Small-Molecule Drug Approvals
In 2022, FDA approved 37 new drugs and biological products classified as new molecular entities (#NMEs). Among these 37 new approvals, there are 20 small molecules (peptide Tirzepatide included), 14 antibody, protein, ADC, and enzyme biological products, 1 chemically modified siRNA drug (Vutrisiran), 1 toxin-based drug (DaxibotulinumotoxinA-lanm), and 1 imaging agent (Hyperpolarized Xe-129).?
#Daridorexant (Quviviq)
An #orexin receptor antagonist indicated for the treatment of adult patients with insomnia is characterized by difficulties with sleep onset and/or sleep maintenance.?
Approval Date：2022/01/07
A selective reversible #JAK1 inhibitor (JAK1 over JAK2, 28-fold; JAK1 over JAK3, >340 fold; JAK1 over TYK2, 43-fold) indicated for the treatment of adults with refractory, moderate-to-severe atopic dermatitis whose disease is not adequately controlled with other systemic drug products, including biologics, or when the use of those therapies is inadvisable.?
Approval Date：2022/01/14
A pyruvate kinase activator is indicated for the treatment of hemolytic anemia in adults with pyruvate kinase deficiency.?
Approval Date：2022/02/17
An oral kinase inhibitor with activity against kinases including wild-type JAK2, mutant JAK2V617F, and FLT3, which contribute to the signaling of a number of cytokines and growth factors that are important for hematopoiesis and immune function. Pacritinib is indicated for the treatment of adults with intermediate or high-risk primary or secondary myelofibrosis with a platelet count below 50 x 109/L.
Approval Date：2022/02/28
#Ganaxolone (Ztalmy)
Indicated for the treatment of seizures associated with CDKL5 deficiency disorder (CDD) in patients over 2 years old. The precise mechanism is unknown, but its anticonvulsant effects may be due to positive allosteric modulation of the GABAA?receptor in the CNS.
Approval Date：2022/03/18
#lutetium (177Lu) vipivotide tetraxetan (Pluvicto)?
A radioligand therapeutic agent containing radionuclide lutetium LU177 which is linked to a moiety that binds to prostate-specific membrane antigen (PSMA), a transmembrane protein that is expressed in prostate cancer, including mCRPC. #Pluvicto is indicated for the treatment of?adult patients with PSMA-positive metastatic castration-resistant prostate cancer (mCRPC) who have been treated with androgen receptor (AR) pathway inhibition and taxane-based chemotherapy.
Approval Date：2022/03/23
An antifungal agent?is indicated to reduce the incidence of recurrent vulvovaginal candidiasis (RVVC) in females with a history of RVVC who are not of reproductive potential.?
Approval Date：2022/04/26
An allosteric and reversible inhibitor selective for cardiac myosin is indicated for the treatment of adults with symptomatic New York Heart Association (NYHA) class II-III obstructive hypertrophic cardiomyopathy (HCM) to improve functional capacity and symptoms.
Approval Date：2022/04/28?
Vonoprazan, Amoxicillin, and Clarithromycin (Voquezna triple pak or Voquezna dual ak)
Vonoprazan suppresses basal and stimulates gastric acid secretion at the secretory surface of the gastric parietal cell through inhibition of the H+, K+-ATPase enzyme system?in a potassium-competitive manner. Amoxicillin is an antibacterial drug. Clarithromycin is a macrolide antimicrobial drug. The drugs are indicated for the treatment of Helicobacter pylori (H. pylori)?infection in adults.?
Approval Date：2022/05/03
A GIP receptor and GLP-1 receptor agonist is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
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Approval Date：2022/05/13
Tapinarof cream, 1% ?(Vtama)?
An aryl hydrocarbon receptor agonist?is indicated for the topical treatment of plaque psoriasis in adults.?
Approval Date：2022/05/23
A TYK2 inhibitor binds to the regulatory domain of TYK2, stabilizing an inhibitory interaction between the regulatory and the catalytic domains of the enzyme, resulting in allosteric inhibition of receptor-mediated activation of TYK2 and its downstream activation of STATs. Sotyktu is indicated for the treatment of moderate-to-severe plaque psoriasis in adults?who are candidates for systemic therapy or phototherapy.
Approval Date：?2022/09/09
A vasopressin receptor agonist?is a 12-amino acid peptide with the chemical name N-[N-(N-glycylglycyl)glycyl]-8-L-lysinevasopressin. Terlivaz is indicated to improve kidney function in adults with hepatorenal syndrome?with a rapid reduction in kidney function.?
Approval Date：2022/09/15
Gadopiclenol (Elucirem)
A gadolinium-based contrast agent which contains gadopiclenol, a paramagnetic macrocyclic non-ionic complex of gadolinium. Elucirem is indicated in adult and pediatric patients of two years old and older for use with MRI to detect and visualize lesions with abnormal vascularity.?
Approval Date：2022/09/21
A relatively selective EP2 receptor agonist?which decreases intraocular pressure is indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.?
Approval Date：2022/09/22
Sodium phenylbutyrate/Taurursodiol (Relyvrio)
Indicated for the treatment of amyotrophic lateral sclerosis (ALS) in adults. The mechanism of action for Relyvrio’s therapeutic effects in ALS patients is unknown.
Approval Date：?2022/09/29?
A kinase inhibitor of FGFR 1, 2, 3, and 4 with IC50?values lower than 4 nM. Futibatinib covalently binds to FGFRs. Lytgobi is indicated for the treatment of adults with previously treated, unresectable, locally advanced, or metastatic intrahepatic cholangiocarcinoma harboring FGFR2 gene functions or other rearrangements.?
Approval Date：2022/09/30
An?inhibitor of mutated isocitrate dehydrogenase-1 (IDH-1)?is indicated for the treatment of adults with relapsed or refractory acute myeloid leukemia (AML) with a susceptible isocitrate dehydrogenase-1 mutation.?
Approval Date：2022/12/01
Adagrasib (Krazati)
An irreversible inhibitor of KRAS G12C that covalently binds to the mutant cysteine in KRAS G12C and locks the mutant #KRAS protein in its inactive state prevents downstream signaling without affecting wild-type KRAS protein. Krazati is indicated for the treatment of adult patients with KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer (NSCLC).?
Approval Date：2022/12/12
An HIV-1 capsid inhibitor is indicated for the treatment of adult patients with HIV whose HIV infections cannot be successfully treated with other available treatments due to resistance, intolerance, or safety considerations. Lenacapavir disrupts HIV capsid protein functions with high potency and long-lasting effects due to its low systemic clearance and slow subcutaneous injection-site release kinetics. Lenacapavir exhibits picomolar antiviral activity against all HIV-1 subtypes tested and shows high synergy and no cross-resistance with approved antiretroviral drugs.
Approval Date：?2022/12/22
postdoctoral researcher ?? medicinal chemist to develop innovative therapeutics
2 年thanks for the insight. Provided hereby are the synthesis for the small molecules approved. https://www.mdpi.com/1999-4923/14/11/2538