{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,7]],"date-time":"2026-09-07T23:46:03Z","timestamp":1788824763750,"version":"build-2803163510"},"reference-count":0,"publisher":"Bentham Science Publishers Ltd.","issue":"1","content-domain":{"domain":["eurekaselect.com"],"crossmark-restriction":true},"short-container-title":["ACAMC"],"published-print":{"date-parts":[[2018,3,16]]},"abstract":"<jats:sec>\n<jats:title\/>\n<jats:p>Objective: Monoclonal antibodies (mAbs) have been radiolabeled with a variety of radioisotopes\nutilizing various kinds of bi-functional chelating agents (BFCAs) with an aim to develop suitable agents for\nradioimmunotherapy. The number of BFCA moieties present per antibody molecule plays a significant role in\ndetermining the pharmacokinetics and immunoreactivity exhibited by the radiolabeled antibodies. The objective\nof the present study is to evaluate the effect of the number of BFCA moieties present per antibody molecule on\nthe pharmacokinetics and immunoreactivity of the 177Lu-labeled Rituximab.\n<\/jats:p><\/jats:sec>\n<jats:sec>\n<jats:title>Methods: <\/jats:title>\n<jats:p>Three different mAb-BFCA conjugates were prepared using different molar ratios of Rituximab\n(mAb) to p-NCS-benzyl-DOTA (BFCA) viz. 1:5, 1:10 and 1:50 employing different reaction conditions.\nStudies were carried out to determine the average number of BFCAs attached per mAb molecule. All the three\nmAb-BFCA conjugates were labeled with 177Lu(III) and were subsequently evaluated in normal Swiss mice to\nascertain their respective pharmacokinetic behavior. In-vitro studies were also performed in Raji cell lines (human\nburkitt's lymphoma) for determining the effect of increasing number of BFCAs attached per mAb molecule\non the immunoreactivity of the resultant 177Lu-labeled mAb-BFCA complexes.\n<\/jats:p><\/jats:sec>\n<jats:sec>\n<jats:title>Results:<\/jats:title>\n<jats:p> 177Lu-labeled mAb-BFCA complex prepared corresponding to 1:50 mAb to BFCA ratio exhibited the\nleast non-specific uptake and rapid clearance from majority of the organs, but also exhibited least immunoreactive\nfraction (IRF = 19.37%). On the other hand, 177Lu-labeled mAb-BFCA complex prepared corresponding\nto 1:5 mAb to BFCA ratio exhibited the highest non-specific uptake and slower clearance pattern, but\nhighest IRF (71.17%). 177Lu-labeled mAb-BFCA complex prepared corresponding to 1:10 mAb:BFCA ratio\nexhibited intermediate pharmacokinetic behaviour with moderate IRF (53.05%).\n<\/jats:p><\/jats:sec>\n<jats:sec>\n<jats:title>Conclusions:<\/jats:title>\n<jats:p> The present study indicates that antibody to BFCA ratio plays a crucial role in determining the\nimmunoreactivity and pharmacokinetic behavior of the radiolabeled antibodies and must be prudently chosen\nfor their successful therapeutic application.<\/jats:p>\n<\/jats:sec>","DOI":"10.2174\/1871520617666170725164530","type":"journal-article","created":{"date-parts":[[2017,7,26]],"date-time":"2017-07-26T12:04:35Z","timestamp":1501070675000},"page":"146-153","update-policy":"https:\/\/doi.org\/10.2174\/bsp_crossmark_policy","source":"Crossref","is-referenced-by-count":16,"title":["Effect of Number of Bifunctional Chelating Agents on the Pharmacokinetics and Immunoreactivity of 177Lu-labeled Rituximab: A Systemic Study"],"prefix":"10.2174","volume":"18","author":[{"given":"Mohini","family":"Guleria","sequence":"first","affiliation":[{"name":"Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Trombay, Mumbai-400 085, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Tapas","family":"Das","sequence":"additional","affiliation":[{"name":"Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Trombay, Mumbai-400 085, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chandan","family":"Kumar","sequence":"additional","affiliation":[{"name":"Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Trombay, Mumbai-400 085, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Rohit","family":"Sharma","sequence":"additional","affiliation":[{"name":"Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Trombay, Mumbai-400 085, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jeyachitra","family":"Amirdhanayagam","sequence":"additional","affiliation":[{"name":"Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Trombay, Mumbai-400 085, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Haladhar D.","family":"Sarma","sequence":"additional","affiliation":[{"name":"Radiation Biology and Health Sciences Division, Bhabha Atomic Research Centre, Trombay, Mumbai-400 085, India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ashutosh","family":"Dash","sequence":"additional","affiliation":[{"name":"Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Trombay, Mumbai-400 085, India"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"965","container-title":["Anti-Cancer Agents in Medicinal Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/eurekaselect.com\/article\/download\/154476","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/www.eurekaselect.com\/154476\/article","content-type":"text\/html","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/eurekaselect.com\/article\/download\/154476","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2020,12,26]],"date-time":"2020-12-26T09:46:42Z","timestamp":1608976002000},"score":1,"resource":{"primary":{"URL":"https:\/\/www.eurekaselect.com\/154476\/article"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2018,3,16]]},"references-count":0,"journal-issue":{"issue":"1","published-print":{"date-parts":[[2018,3,16]]}},"alternative-id":["LiveAll1"],"URL":"https:\/\/doi.org\/10.2174\/1871520617666170725164530","relation":{},"ISSN":["1871-5206"],"issn-type":[{"value":"1871-5206","type":"print"}],"subject":[],"published":{"date-parts":[[2018,3,16]]},"assertion":[{"value":"Peer Reviewed","order":0,"name":"review_status","label":"Review Status","group":{"name":"peer_review_details","label":"Peer Review Details"}},{"value":"Single blind","order":1,"name":"review_process","label":"Review Process","group":{"name":"peer_review_details","label":"Peer Review Details"}},{"value":"Checked with iThenticate","order":0,"name":"screening_status","label":"Screening Status","group":{"name":"plagiarism_screening","label":"Plagiarism Screening"}},{"value":"2017-02-08","order":0,"name":"received","label":"Received","group":{"name":"publication_history","label":"Publication History"}},{"value":"2017-05-30","order":1,"name":"revised","label":"Revised","group":{"name":"publication_history","label":"Publication History"}},{"value":"2017-07-19","order":2,"name":"accepted","label":"Accepted","group":{"name":"publication_history","label":"Publication History"}},{"value":"2018-03-16","order":3,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}]}}