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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