| Chemical Properties | Back Directory | [form ]
Solid | [color ]
White to off-white | [Sequence]
{D-Tyr}-Ile-Cys-Val-{Trp(Me)}-Gln-Asp-Trp-{Sar}-Ala-His-Arg-Cys-{N(Me)Ile}-NH2 (Disulfide bridge:Cys3-Cys13) |
| Hazard Information | Back Directory | [Uses]
AMY-101 TFA (Cp40 TFA), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation[1][2]. | [in vivo]
AMY-101 can improve the periodontal condition of NHPs with natural chronic periodontitis[1].
AMY-101 can induce a long-lasting anti-inflammatory effect[1].
AMY-101 (4 mg/kg bodyweight, subcutaneous injection. once per 24 hr for a total of 28 days) causes a significant and long-lasting reduction in PPD, an index that measures tissue destruction[1].
AMY-101 (Cp40, 1 mg/kg, sc, injection every 12 h, daily, 7 or 14 days) attenuates fibrosis and infiltration of inflammatory cells in UUO-induced renal fibrosis[3]. | Animal Model: | Fifteen adult male cynomolgus monkeys (Macaca fascicularis) (7-15 years old; 5.0-7.6 kg body weight)[1]. | | Dosage: | 0.1 mg/site; 50 μL of 2 mg/mL solution. | | Administration: | Injected locally. (Either three times per week or once a week for 6 weeks followed by a 6-week follow-up period without treatment.) | | Result: | Does not cause irritation in healthy gingiva. |
| Animal Model: | UUO and sham-operated mice[3]. | | Dosage: | 1 mg/kg. | | Administration: | Subcutaneous injection every 12 h, daily, 7 or 14 days. | | Result: | 1 mg/kg Cp40 had much less severe interstitial fibrosis than control peptide-injected mice. |
| [References]
[1] Kajikawa T, et al. Safety and Efficacy of the Complement Inhibitor AMY-101 in a Natural Model of Periodontitis in Non-human Primates. Mol Ther Methods Clin Dev. 2017 Aug 18;6:207-215. DOI:10.1016/j.omtm.2017.08.001
[2] Mastaglio S, et al. The first case of COVID-19 treated with the complement C3 inhibitor AMY-101. Clin Immunol. 2020 Apr 29:108450. DOI:10.1016/j.clim.2020.108450
[3] Yanyan Liu, et al. Complement C3 Produced by Macrophages Promotes Renal Fibrosis via IL-17A Secretion. Front Immunol. 2018 Oct 22;9:2385. DOI:10.3389/fimmu.2018.02385 |
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