{"id":594,"date":"2015-12-08T15:31:25","date_gmt":"2015-12-08T15:31:25","guid":{"rendered":"http:\/\/caltagmedsystems.co.uk\/information\/?p=594"},"modified":"2023-07-04T15:27:09","modified_gmt":"2023-07-04T15:27:09","slug":"silensomes-one-single-model-for-dmpk-phenotyping-studies","status":"publish","type":"post","link":"https:\/\/www.caltagmedsystems.co.uk\/information\/silensomes-one-single-model-for-dmpk-phenotyping-studies\/","title":{"rendered":"Silensomes: One single model for DMPK phenotyping studies"},"content":{"rendered":"

Silensomes™ are human pooled liver microsomes in which one\u00a0specific CYP has been chemically knocked out and are capable of directly\u00a0quantifying and predicting the contribution of CYP enzymes in drug metabolism.<\/span><\/p>\n

Until now, a battery of in-vitro tests recommended by the\u00a0regulatory agencies (EMA\/FDA) are required for this CYP phenotyping assay. These\u00a0tests (correlation analysis, antibody or chemical inhibition and metabolism by\u00a0recombinant human enzymes) have a number of disadvantages:<\/span><\/p>\n

– No direct quantitative measurement of the contribution of\u00a0each CYP in the metabolism of a drug (correlation analysis)
\n<\/span>– Model is not fully representative of the liver enzyme\u00a0profile (e.g. human recombinant CYP450)
\n<\/span>– Lack of specificity (e.g. anti-CYP antibodies and chemical\u00a0inhibitors)<\/span><\/p>\n

To overcome the disadvantages of the current methodologies,\u00a0Biopredic International<\/a> has developed a patented new in-vitro drug development model.<\/span><\/p>\n

Silensomes™<\/a> are validated human pooled liver microsomes (HLMs)\u00a0chemically and irreversibly inactivated for one specific CYP using mechanism\u00a0based inhibitors (MBI). <\/span><\/p>\n

Each Silensomes™ is available as ready-to-use HLMs\u00a0chemically knocked-out for one specific CYP activity (1A2, 2A6, 2B6, 2C8, 2C9,\u00a02C19, 2D6, 2E1, 3A4) with each showing high specificity and efficiency of their\u00a0targeted CYP inhibition (>80%), and only minor impact (<20%),<\/span><\/p>\n

Key Advantages of Silensomes™:<\/span><\/b><\/p>\n

– Silensomes™: the model of choice for determination of the\u00a0CYP contribution all along the development plan of a new chemical entity
\n<\/span>– Irreversibly inhibited CYPs
\n– For initial rate conditions
\n– For saturating conditions
\n– One single model for CYP phenotyping assays, instead of a\u00a0battery of in-vitro tests
\n<\/span>– Quantitative: the true contribution of the CYP450 in the\u00a0metabolism of the compound can be measured
\n<\/span>– A powerful model with an excellent specificity, potency,\u00a0stability and predictability to ensure reliable extrapolation of the drug-drug\u00a0<\/span>interaction risk
\n<\/span>– More representative of in-vivo, using human liver microsomes\u00a0rather than recombinant enzymes isolated from non-mammalian cells<\/span><\/p>\n

Silensomes™<\/a> are available for compound screening purposes\u00a0and also for regulatory validation<\/span><\/p>\n

Silensomes are now available for beta testing. Please contact us<\/a> if you would be\u00a0interested in this.<\/span>
\n<\/span><\/p>\n

Caltag Medsystems <\/span><\/a>is the distributor of Biopredic<\/span> <\/a>products in the UK and Ireland. If you have any questions about these products, please contact<\/span><\/a> us<\/span><\/a>.<\/p>\n","protected":false},"excerpt":{"rendered":"

Silensomes™ are human pooled liver microsomes in which one\u00a0specific CYP has been chemically knocked out and are capable of directly\u00a0quantifying and predicting the contribution of CYP enzymes in drug metabolism. Until now, a battery of in-vitro tests recommended by the\u00a0regulatory<\/p>\n","protected":false},"author":13,"featured_media":0,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[18],"tags":[],"class_list":["post-594","post","type-post","status-publish","format-standard","hentry","category-cell-culture"],"_links":{"self":[{"href":"https:\/\/www.caltagmedsystems.co.uk\/information\/wp-json\/wp\/v2\/posts\/594","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/www.caltagmedsystems.co.uk\/information\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/www.caltagmedsystems.co.uk\/information\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/www.caltagmedsystems.co.uk\/information\/wp-json\/wp\/v2\/users\/13"}],"replies":[{"embeddable":true,"href":"https:\/\/www.caltagmedsystems.co.uk\/information\/wp-json\/wp\/v2\/comments?post=594"}],"version-history":[{"count":3,"href":"https:\/\/www.caltagmedsystems.co.uk\/information\/wp-json\/wp\/v2\/posts\/594\/revisions"}],"predecessor-version":[{"id":7572,"href":"https:\/\/www.caltagmedsystems.co.uk\/information\/wp-json\/wp\/v2\/posts\/594\/revisions\/7572"}],"wp:attachment":[{"href":"https:\/\/www.caltagmedsystems.co.uk\/information\/wp-json\/wp\/v2\/media?parent=594"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.caltagmedsystems.co.uk\/information\/wp-json\/wp\/v2\/categories?post=594"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/www.caltagmedsystems.co.uk\/information\/wp-json\/wp\/v2\/tags?post=594"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}