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Technetium (^99mTc) arcitumomab is a drug used for the diagnostic imaging of colorectal cancers, marketed by Immunomedics.^[1] 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.

Before application, arcitumomab is reconstituted with a solution of the radioactive agent sodium pertechnetate (^99mTc) from a technetium generator.^[1]

Mechanism of action

Arcitumomab recognizes carcinoembryonic antigen (CEA), an antigen over-expressed in 95% of colorectal cancers.^[2] Consequently, the antibody accumulates in such tumours together with the radioisotope, which emits photons. Via single photon emission computed tomography (SPECT), high-resolution images showing localisation, remission or progression, and metastases of the tumour can be obtained.^[1]^[3]

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.^[1]

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 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.^[1]

Radioactivity can lead to radiation poisoning. Since the dose of an arcitumomab application is about 10 mSv,^[1] such an overdose is unlikely.

References

^ ^a ^b ^c ^d ^e ^f "CEA-Scan Summary of Product Characteristics". Immunomedics.
^ Guadagni, Fiorella; Kantor, J; Aloe, S; Carone, MD; Spila, A; D'alessandro, R; Abbolito, MR; Cosimelli, M et al. (15 March 2001). "Detection of Blood-borne Cells in Colorectal Cancer Patients by Nested Reverse Transcription-Polymerase Chain Reaction for Carcinoembryonic Antigen Messenger RNA". Cancer Research 61 (6): 2523–32. PMID 11289125.
^ Behr, T; Becker, W; Hannappel, E; Goldenberg, DM; Wolf, F (1995). "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". Cancer Research 55 (23 Suppl): 5777s–5785s. PMID 7493346.

English Journal

In vivo near-infrared fluorescence imaging of carcinoembryonic antigen-expressing tumor cells in mice.

Lisy MR, Goermar A, Thomas C, Pauli J, Resch-Genger U, Kaiser WA, Hilger I.SourceInstitute for Diagnostic and Interventional Radiology, Friedrich-Schiller-University Jena, FZL Erlanger Allee 101, D-07747 Jena, Germany.
Radiology.Radiology.2008 Jun;247(3):779-87. Epub 2008 Apr 15.
PURPOSE: To prospectively depict carcinoembryonic antigen (CEA)-expressing tumors in mice with a high-affinity probe consisting of a near-infrared (NIR) fluorochrome and the clinically used anti-CEA antibody fragment arcitumomab.MATERIALS AND METHODS: This study was approved by the regional animal c
PMID 18413884

[Personal experience using radioimmunoguided surgery (RIGS)].

Gioffrè Florio MA, Famà F, Gullo G, Mazzei S, Pollicino A, Scarfò P, Vindigni A.SourceChirurgia Generale, Policlinico Universitario G. Martino, Messina.
Annali italiani di chirurgia.Ann Ital Chir.2007 Sep-Oct;78(5):433-7.
Radio Immuno Guided Surgery (RIGS) is a technique that has numerous uses in oncology. It is characterised by a multidisciplinary approach by nuclear physician and surgeon for diagnosis and treatment; it uses colloid radiotracers, monoclonal antibodies or non-immunological tracers. We adopted this te
PMID 18338553

Japanese Journal

A prospective study of 2-[18F] Fluoro-2-Deoxy-D-Glicose/positron emission tomography scan, 99m Tclabeled Arcitumomab (CEA-scan), and blind second-look laparotomy for detecting colon cancer recurrence in patients with increasing carcinoembryonic antigen levels

Ann Surg Oncol 8, 779-786, 2001
NAID 30022811670

「mab」

Technetium (^99mTc) arcitumomab^?
Monoclonal antibody
Type	Fab' fragment
Source	Mouse
Target	CEA
Clinical data
Pregnancy; category	US: C (Risk not ruled out);
Legal status	℞ (Prescription only);
Routes of; administration	Intravenous
Pharmacokinetic data
Bioavailability	N/A
Biological half-life	13 ± 4 hours
Identifiers
CAS Registry Number	154361-48-5 (arcitumomab)
ATC code	V09IA06
UNII	029JF1SCU8
Chemical data
Molecular mass	ca. 50 kDa
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関: モノクローナル抗体

mab

abciximab
adahmumab
adalimumab
afelimomab
alemtuzumab
apolizumab
arcitumomab
basiliximab
bevacizumab
cantuzumab
certolizumab
cetolizumab
cetuximab
clenoliximab
daclizumab
デノスマブ denosumab 抗RANKL抗体
eculizumab
edrecolomab
efalizumab
epratuzumab
galiximab
gemtuzumab
ibritumomab
インフリキシマブ infliximab 抗TNF-α抗体クローン病 Ph⁺ALL
inotuzumab
keliximab
natalizumab
nebacumab
omalilzumab
omalizumab
oregovomab
palivizumab
panitumumab
pertuzumab
pexelizumab
リツキシマブ rituximab：抗CD20抗体：慢性リンパ性白血病、B細胞リンパ腫

[SPC-1] ^ ^a ^b ^c ^d ^e ^f "CEA-Scan Summary of Product Characteristics". Immunomedics.

[2] Guadagni, Fiorella; Kantor, J; Aloe, S; Carone, MD; Spila, A; D'alessandro, R; Abbolito, MR; Cosimelli, M et al. (15 March 2001). "Detection of Blood-borne Cells in Colorectal Cancer Patients by Nested Reverse Transcription-Polymerase Chain Reaction for Carcinoembryonic Antigen Messenger RNA". Cancer Research 61 (6): 2523–32. PMID 11289125.

[3] Behr, T; Becker, W; Hannappel, E; Goldenberg, DM; Wolf, F (1995). "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". Cancer Research 55 (23 Suppl): 5777s–5785s. PMID 7493346.

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arcitumomab