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Pharmacokinetics of
Radiopharmaceuticals
Oncology
Report by: Nicole Mae D.C. Martinez
Radiopharmaceuticals
(67Ga) Gallium citrate
(201Tl) Thallous chloride
Outline
Background
Clinical Use
Administration
Mechanism of Action
Distribution
Excretion

(67Ga) Gallium citrate

Physical Half-life: 78.3 h
Gamma emitter: 185 and 300 keV
Activity administered: 80 150 MBq (2-3 mCi)
Effective dose equivalent: 17 mSv (1700 mrem)

(67Ga) Gallium citrate

Clinical Uses: Hodgkins disease, lymphomas,
melanoma, hepatoma, head & neck tumors,
tumor masses > 1 cm, bronchogenic carcinoma
and mediastinal metastatic diseases

(67Ga) Gallium citrate

Administration: Intravenous Injection

Mechanism of Action: Ga-67 citrate is
transported by the blood by bounding to
plasma proteins, mainly transferrin, which is
the main protein in the blood that binds to
iron.

(67Ga) Gallium citrate

Gallium is taken up into sites with tumor,
inflammation and infection.

The 67Ga transferrin complex binds to the
receptors on cell membranes. Increased
capillary permeability facilitates Ga-67 entry
into the sites with tumor, inflammation and
infection.

(67Ga) Gallium citrate

Distribution: Blood pool activity remains high
for up to 24 h. Beyond 48 h, most of Ga-67 is
cell bound.

Excretion: The average whole body retention
is 65 percent after seven days, with 26
percent having been excreted in the urine and
9 percent in the stools.



(201Tl) Thallous chloride


Physical Half-life: 72.9 h
Gamma emitter: 135.3 and 167.4 keV
Activity administered: 74 185 MBq (2-5 mCi)



(201Tl) Thallous chloride


Clinical Uses: Brain tumors, bone tumors,
medullary thyroid carcinoma, and various other
tumors.

Administration: Intravenous Injection



(201Tl) Thallous chloride


Mechanism of Action: Thallium acts as a
potassium analogue, enabling it to transfer
across the cellular membrane. It is kept
intracellular by the Na/K ATP pump.




(201Tl) Thallous chloride


Distribution: 5 mins after IV injection, only 5
8 % of injected activity remains in the blood.

Excretion: Approximately 4 - 8 % of the
injected dose was excreted in the urine in the
first 24 hours. The whole body disappearance
half-time was 9.8 2.5 days.

References
Sharp, P. & Gemmell, H. (2005). Practical Nuclear Medicine (3rd ed.).
London City, London: Springer.
http://www.drugs.com/pro/gallium-citrate-ga-67.html
http://www.druginformation.com/RxDrugs/G/Gallium%20Citrate%20Ga%206
7%20Injection.html#Kinetics
Nuclear Hepatology: A Textbook of Hepatobiliary Diseases by Gerbail T.
Krishnamurthy, S. Krishnamurthy
http://www.drugs.com/pro/thallous-chloride.html
Imaging of Brain Tumors with Histological Correlations by Antonios
Drevelegas