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Cytosine arabinoside binding to human plasma proteins
Archives Internationales De Pharmacodynamie Et De Therapie
|October 1, 1977
Summary
Cytosine arabinoside (Ara-C) interacts with human plasma proteins, with approximately 13.3% of the drug bound to proteins within the therapeutic concentration range. This binding percentage remained consistent across studied levels.
Area of Science:
- Pharmacology
- Biochemistry
Background:
- Cytosine arabinoside (Ara-C) is a chemotherapy agent used in treating various cancers.
- Understanding drug-protein interactions is crucial for predicting drug efficacy and pharmacokinetics.
Purpose of the Study:
- To quantify the extent of cytosine arabinoside (Ara-C) binding to human plasma proteins.
- To determine if Ara-C binding is concentration-dependent within the therapeutic range.
Main Methods:
- Ultrafiltration
- Ultracentrifugation
Main Results:
- Both ultrafiltration and ultracentrifugation yielded comparable results.
- Approximately 13.3% (SD: 2.2%) of Ara-C in human plasma was found to be bound to proteins.
- The percentage of protein-bound Ara-C was independent of drug concentration within the therapeutic range (0.005-1.0 mg/l).
Conclusions:
- Ara-C exhibits a moderate level of binding to human plasma proteins.
- The binding characteristics of Ara-C suggest predictable pharmacokinetic behavior within its therapeutic dosage.
- Further studies may explore the specific plasma proteins involved in Ara-C binding.