PMC:7795856 / 13190-14269 JSONTXT

{"target":"https://pubannotation.org/docs/sourcedb/PMC/sourceid/7795856","sourcedb":"PMC","sourceid":"7795856","source_url":"https://www.ncbi.nlm.nih.gov/pmc/7795856","text":"To mimic the clinically approved route of Zadaxin™ administration, the N-acetylated Tα1-PAS was injected subcutaneously into the dorsal area of rats (N = 5). The injected dose of 3.4 mg/kg Tα1-PAS was well tolerated without any drug-related adverse events or significant changes in body weight. The Tα1-PAS plasma levels at various sampling times were analyzed using a quantitative sandwich ELISA developed to detect only Tα1-PAS and no endogenous rat Tα1, which shares 100% sequence identity with the human peptide. The pharmacokinetic (PK) profile of Tα1-PAS (Figure 4) exhibited a typical curve according to the Bateman function [40], with a Cmax of 25.6 ± 4.4 mg/L at tmax = 22.7 ± 1.1 h. Curve fitting with the WinNonlin software revealed a drastically extended terminal half-life of 15.9 ± 0.9 h, which is more than 8-fold longer than the one for the native peptide (τ1/2 = 1.9 h) published for rats [41]. The strong impact of PASylation on the PK profile is also reflected by other parameters such as the large area under the curve (AUC) and slow clearance (CL) (Table 1).","tracks":[{"project":"LitCovid-PubTator","denotations":[{"id":"252","span":{"begin":299,"end":302},"obj":"Gene"},{"id":"253","span":{"begin":452,"end":455},"obj":"Gene"},{"id":"254","span":{"begin":144,"end":148},"obj":"Species"},{"id":"255","span":{"begin":448,"end":451},"obj":"Species"},{"id":"256","span":{"begin":502,"end":507},"obj":"Species"},{"id":"257","span":{"begin":901,"end":905},"obj":"Species"},{"id":"258","span":{"begin":71,"end":91},"obj":"Chemical"},{"id":"259","span":{"begin":189,"end":196},"obj":"Chemical"}],"attributes":[{"id":"A252","pred":"tao:has_database_id","subj":"252","obj":"Gene:50719"},{"id":"A253","pred":"tao:has_database_id","subj":"253","obj":"Gene:50719"},{"id":"A254","pred":"tao:has_database_id","subj":"254","obj":"Tax:10116"},{"id":"A255","pred":"tao:has_database_id","subj":"255","obj":"Tax:10116"},{"id":"A256","pred":"tao:has_database_id","subj":"256","obj":"Tax:9606"},{"id":"A257","pred":"tao:has_database_id","subj":"257","obj":"Tax:10116"},{"subj":"252","pred":"source","obj":"LitCovid-PubTator"},{"subj":"253","pred":"source","obj":"LitCovid-PubTator"},{"subj":"254","pred":"source","obj":"LitCovid-PubTator"},{"subj":"255","pred":"source","obj":"LitCovid-PubTator"},{"subj":"256","pred":"source","obj":"LitCovid-PubTator"},{"subj":"257","pred":"source","obj":"LitCovid-PubTator"},{"subj":"258","pred":"source","obj":"LitCovid-PubTator"},{"subj":"259","pred":"source","obj":"LitCovid-PubTator"}],"namespaces":[{"prefix":"Tax","uri":"https://www.ncbi.nlm.nih.gov/taxonomy/"},{"prefix":"MESH","uri":"https://id.nlm.nih.gov/mesh/"},{"prefix":"Gene","uri":"https://www.ncbi.nlm.nih.gov/gene/"},{"prefix":"CVCL","uri":"https://web.expasy.org/cellosaurus/CVCL_"}]},{"project":"LitCovid-sentences","denotations":[{"id":"T81","span":{"begin":0,"end":157},"obj":"Sentence"},{"id":"T82","span":{"begin":158,"end":294},"obj":"Sentence"},{"id":"T83","span":{"begin":295,"end":516},"obj":"Sentence"},{"id":"T84","span":{"begin":517,"end":692},"obj":"Sentence"},{"id":"T85","span":{"begin":693,"end":911},"obj":"Sentence"},{"id":"T86","span":{"begin":912,"end":1079},"obj":"Sentence"}],"namespaces":[{"prefix":"_base","uri":"http://pubannotation.org/ontology/tao.owl#"}],"attributes":[{"subj":"T81","pred":"source","obj":"LitCovid-sentences"},{"subj":"T82","pred":"source","obj":"LitCovid-sentences"},{"subj":"T83","pred":"source","obj":"LitCovid-sentences"},{"subj":"T84","pred":"source","obj":"LitCovid-sentences"},{"subj":"T85","pred":"source","obj":"LitCovid-sentences"},{"subj":"T86","pred":"source","obj":"LitCovid-sentences"}]}],"config":{"attribute types":[{"pred":"source","value type":"selection","values":[{"id":"LitCovid-PubTator","color":"#ec93bb","default":true},{"id":"LitCovid-sentences","color":"#93d6ec"}]}]}}