약학회지

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Table. 1.

Table. 1. 2023 FDA-approved peptide drugs in 2023
INN name (Brand name) Date of approval Structural characteristics Pharmacokinetics Mode of action Indication
Trofinetide (DaybueTM) 2023/03/10 IGF-1 N-terminal tripeptide derivative with a methyl group at the proline alpha position for improved stability p.o.; BA 84%; Tmax 2-3 h; Vd 80 L; PPB <6%; t½ 1.5 h Uncleara Rett syndromeb
Rezafungin (RezzayoTM) 2023/03/22 Echinocandin B derivative of cyclic hexapeptide with a choline aminal ether for improved stability and solubility i.v.; Vd 67 L; PPB 95.6%; CL 0.35 L/h; t½ 152 h 1,3-β-D-glucan synthase inhibitor Candidemia and invasive candidiasisc
Flotufolastat F 18 (PoslumaTM) 2023/05/25 Radiohybrid with urea-based PSMA ligand, 18F-labeled SiFA and DOTAGA complex Stable up to 50 min after i.v.; distributes to liver (15.8%), heart blood pool (7.4%), and kidney (3.2%); 7% and 15% excreted in the urine in the first 2 and 4.5 h post-injection, respectively. PSMA-PET imaging agent Prostate cancer diagnosisd
Nirmatrelvir/Ritonavir (PaxlovidTM) 2023/05/25 Peptidomimetic inhibitor with various modificationsa p.o.; for nirmatrelvir given with ritonavir, Tmax 3 h; Vd,ss 104.7 L; PPB 69%; CL 8.99 L/h; t½ 6.05 h SARS-CoV-2 main protease covalent inhibitor/CYP3A and HIV-1 protease inhibitor Mild-to-moderate COVID-19
Motixafortide (AphexdaTM) 2023/09/08 Polyphemusin II derivative with various modificationsa s.c.; Tmax 0.25-1.17 h; Vd 27 L; PPB >99%; CL 46.5 L/h; t½ 2 h CXCR4 antagonist Hematopoietic stem cell mobilizer in patients with multiple myelomae
Tirzepatide (ZepboundTM) 2023/11/08 GIP derivative with C20 fatty diacid for improved PPB and metabolic stability s.c.; Tmax 8-72 h; Vd,ss 9.7 L; PPB 99%; CL 0.056 L/h; t½ 5 d GIP/GLP-1 receptors dual agonist Adults with obesityf or overweightg, and with weightrelated medical problemsh to lose weight and keep it off

aSee, text for details. bIn adults and pediatric patients 2 years of age and older. cPatients 18 years of age or older who have limited or no alternative options. dImaging PSMA positive lesions. eIndicated in combination with filgrastim to mobilize hematopoietic stem cells to the periphenral blood for collection and subsequent autologous transplantation fwith a BMI of 30 kg/m2 or greater gwith a BMI of 27 kg/m2 or greater hSuch as hypertension, dyslipidemia, type 2 diabetes mellitus, obstructive sleep apnea or cardiovascular disease.

Yakhak Hoeji 2024;68:79-83 https://doi.org/10.17480/psk.2024.68.2.79
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