PMC:7795856 / 13127-14269 JSONTXT

{"project":"LitCovid-PubTator","denotations":[{"id":"243","span":{"begin":34,"end":37},"obj":"Gene"},{"id":"252","span":{"begin":362,"end":365},"obj":"Gene"},{"id":"253","span":{"begin":515,"end":518},"obj":"Gene"},{"id":"254","span":{"begin":207,"end":211},"obj":"Species"},{"id":"255","span":{"begin":511,"end":514},"obj":"Species"},{"id":"256","span":{"begin":565,"end":570},"obj":"Species"},{"id":"257","span":{"begin":964,"end":968},"obj":"Species"},{"id":"258","span":{"begin":134,"end":154},"obj":"Chemical"},{"id":"259","span":{"begin":252,"end":259},"obj":"Chemical"}],"attributes":[{"id":"A243","pred":"tao:has_database_id","subj":"243","obj":"Gene:50719"},{"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"}],"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_"}],"text":"2.3. PASylation Strongly Prolongs Tα1 Pharmacokinetics in Rats\nTo 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)."}

{"project":"LitCovid-sentences","denotations":[{"id":"T79","span":{"begin":0,"end":4},"obj":"Sentence"},{"id":"T80","span":{"begin":5,"end":62},"obj":"Sentence"},{"id":"T81","span":{"begin":63,"end":220},"obj":"Sentence"},{"id":"T82","span":{"begin":221,"end":357},"obj":"Sentence"},{"id":"T83","span":{"begin":358,"end":579},"obj":"Sentence"},{"id":"T84","span":{"begin":580,"end":755},"obj":"Sentence"},{"id":"T85","span":{"begin":756,"end":974},"obj":"Sentence"},{"id":"T86","span":{"begin":975,"end":1142},"obj":"Sentence"}],"namespaces":[{"prefix":"_base","uri":"http://pubannotation.org/ontology/tao.owl#"}],"text":"2.3. PASylation Strongly Prolongs Tα1 Pharmacokinetics in Rats\nTo 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)."}