Binding competitors for use in macrophilin-binding pharmaceutical assays and methods of use thereof

A method of determining the presence of a macrophilin-binding pharmaceutical in a sample, the method comprising the steps of:

• adding to the sample a binding competitor to displace the macrophilin-binding pharmaceutical from its immunophilin complexes, wherein the binding competitor is at least one of:
• (a) the compound represented by Formula IV:
• (b) the compound represented by Formula V:
• (c) the compound represented by Formula VI:
• or
• (d) the compound represented by Formula VII:
• adding a macrophilin-binding pharmaceutical-specific binding partner that binds to the pharmaceutical to form a binding partner/pharmaceutical complex, and wherein the binding partner does not significantly bind to the binding competitor;
• and
• detecting the binding partner/pharmaceutical complex and correlating the detection with an amount of pharmaceutical present in the sample.

A kit for the detection of the presence of a macrophilin-binding pharmaceutical in a sample, the kit comprising:

• a binding competitor that displaces the macrophilin-binding pharmaceutical from its immunophilin complexes, wherein the binding competitor is at least one of:
• (a) the compound represented by Formula IV:
• (b) the compound represented by Formula V:
• (c) the compound represented by Formula VI:
• or
• (d) the compound represented by Formula VII:
• and
• a macrophilin-binding pharmaceutical-specific binding partner that binds to the pharmaceutical for detection of a binding partner/pharmaceutical complex, and wherein the binding partner does not significantly bind to the binding competitor.