Wikipedia:WikiProject Chemicals/Chembox validation/VerifiedDataSandbox and Technetium (99mTc) arcitumomab: Difference between pages

{{Short description|Pharmaceutical drug}}

{{DISPLAYTITLE:Technetium (^99mTc) arcitumomab}}

| verifiedrevid = 470478168

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| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}

| ChemSpiderID = none

| CAS_number_Ref = {{cascite|correct|CAS}}

| CAS_number = 154361-49-6

| UNII_Ref = {{fdacite|correct|FDA}}

| UNII = 029JF1SCU8

| DrugBank = DB00113

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| molecular_weight = 54

| molecular_weight_comment = kDa{{cn|date=December 2023}}

'''Technetium (^99mTc) arcitumomab''' is a drug used for the diagnostic imaging of [[colorectal cancer]]s, marketed by [[Immunomedics]].<ref name="SPC">{{cite web|url=http://www.cea-scan.com/inserts/epckginst.htm|title=CEA-Scan Summary of Product Characteristics|publisher=Immunomedics|access-date=2009-10-28|archive-date=2016-03-13|archive-url=https://web.archive.org/web/20160313061725/http://cea-scan.com/inserts/epckginst.htm|url-status=dead}}</ref> It consists of the [[Fab' fragment]] of a [[monoclonal antibody]] (arcitumomab, trade name '''CEA-Scan''') and a [[radionuclide]], [[technetium-99m]].

==Chemistry==

Technetium (^99mTc) arcitumomab is an [[immunoconjugate]]. Arcitumomab is a Fab' fragment of IMMU-4, a [[murine]] [[IgG1]] monoclonal antibody extracted from the [[ascites]] of mice. The enzyme [[pepsin]] cleaves the F(ab')₂ fragment off the antibody. From this, the Fab' fragment is prepared by mild [[reduction (chemistry)|reduction]].

Before application, arcitumomab is reconstituted with a solution of the radioactive agent sodium [[pertechnetate]] (^99mTc) from a [[technetium generator]].<ref name="SPC" />

==Mechanism of action==

Arcitumomab recognizes [[carcinoembryonic antigen]] (CEA), an antigen over-[[Expression (genetics)|expressed]] in 95% of colorectal cancers.<ref>{{cite journal | vauthors = Guadagni F, Kantor J, Aloe S, Carone MD, Spila A, D'Alessandro R, Abbolito MR, Cosimelli M, Graziano F, Carboni F, Carlini S, Perri P, Sciarretta F, Greiner JW, Kashmiri SV, Steinberg SM, Roselli M, Schlom J | display-authors = 6 | title = Detection of blood-borne cells in colorectal cancer patients by nested reverse transcription-polymerase chain reaction for carcinoembryonic antigen messenger RNA: longitudinal analyses and demonstration of its potential importance as an adjunct to multiple serum markers | journal = Cancer Research | volume = 61 | issue = 6 | pages = 2523–32 | date = March 2001 | pmid = 11289125 | url = http://cancerres.aacrjournals.org/cgi/content/abstract/61/6/2523 }}</ref> Consequently, the antibody accumulates in such tumours together with the radioisotope, which emits [[photon]]s. Via [[single photon emission computed tomography]] (SPECT), high-resolution images showing localisation, [[remission (medicine)|remission]] or progression, and [[metastases]] of the tumour can be obtained.<ref name="SPC" /><ref>{{cite journal | vauthors = Behr T, Becker W, Hannappel E, Goldenberg DM, Wolf F | title = Targeting of liver metastases of colorectal cancer with IgG, F(ab')2, and Fab' anti-carcinoembryonic antigen antibodies labeled with 99mTc: the role of metabolism and kinetics | journal = Cancer Research | volume = 55 | issue = 23 Suppl | pages = 5777s–5785s | date = December 1995 | pmid = 7493346 }}</ref>

==Contraindications==

Technetium (^99mTc) arcitumomab is [[contraindicated]] for patients with known allergies or hypersensitivity to mouse proteins, as well as during pregnancy. Women should pause breast feeding for 24 hours after application of the drug.<ref name="SPC" />

==Adverse effects and overdose==

Only mild and transient side effects have been observed, mostly immunological reactions like [[eosinophilia]], itching and fever. Some patients develop [[Human anti-mouse antibody|human anti-mouse antibodies]], so there is the theoretical possibility of [[anaphylactic reactions]]. High doses of IMMU-4 (up to 20-fold diagnostic arcitumomab dose) have not led to any serious events. One patient has been reported to develop a [[grand mal]] after application.<ref name="SPC" />

Radioactivity can lead to [[radiation poisoning]]. Since the dose of an arcitumomab application is about 10 m[[Sievert|Sv]],<ref name="SPC" /> such an overdose is unlikely.

== References ==

{{reflist}}

== Further reading ==

{{refbegin}}

* {{cite journal | vauthors = Primus FJ, Newell KD, Blue A, Goldenberg DM | title = Immunological heterogeneity of carcinoembryonic antigen: antigenic determinants on carcinoembryonic antigen distinguished by monoclonal antibodies | journal = Cancer Research | volume = 43 | issue = 2 | pages = 686–92 | date = February 1983 | pmid = 6184152 }}

* {{cite journal | vauthors = Hansen HJ, Jones AL, Sharkey RM, Grebenau R, Blazejewski N, Kunz A, Buckley MJ, Newman ES, Ostella F, Goldenberg DM | display-authors = 6 | title = Preclinical evaluation of an "instant" 99mTc-labeling kit for antibody imaging | journal = Cancer Research | volume = 50 | issue = 3 Suppl | pages = 794s–798s | date = February 1990 | pmid = 2297726 }}

* {{cite journal| vauthors = Hughes K |title=Use of radioimmunodetection with CEAScan in planning for resection of recurrent colorectal cancer|journal=Proc Amer Soc Clin Oncol|volume=14|year=1995|page=544}}

* {{cite journal | vauthors = Moffat FL, Pinsky CM, Hammershaimb L, Petrelli NJ, Patt YZ, Whaley FS, Goldenberg DM | title = Clinical utility of external immunoscintigraphy with the IMMU-4 technetium-99m Fab' antibody fragment in patients undergoing surgery for carcinoma of the colon and rectum: results of a pivotal, phase III trial. The Immunomedics Study Group | journal = Journal of Clinical Oncology | volume = 14 | issue = 8 | pages = 2295–305 | date = August 1996 | pmid = 8708720 | doi = 10.1200/JCO.1996.14.8.2295 }}

{{refend}}

{{Radiopharmaceuticals}}

{{Monoclonals for tumors}}

{{DEFAULTSORT:Technetium (99mtc) Arcitumomab}}

[[Category:Radiopharmaceuticals]]

[[Category:Technetium-99m]]

[[Category:Technetium compounds]]

[[Category:Antibody-drug conjugates]]

[[Category:Monoclonal antibodies for tumors]]