ZB716
ZB716' is a synthetic, steroidal, orally active antiestrogen that is currently under development for the treatment of estrogen receptor (ER)-positive metastatic breast cancer. It acts as a silent antagonist of the ERα (IC50 = 4.1 nM) and is also classified as a selective estrogen receptor degrader (SERD). ZB716 is an analogue and prodrug of fulvestrant, distinguished by the substitution of the C3 hydroxyl group with a boronic acid moiety, which contributes to its oral bioavailability.
Pronunciation
ZB Seven-One-Six
Etymology
The name ZB716 does not have a publicly disclosed etymology. It is a code name used in the development phase to identify this particular compound. The designation "fulvestrant-3-boronic acid" suggests its chemical relationship with fulvestrant, featuring a boronic acid modification.
Pharmacodynamics
ZB716 is a potent antagonist of the estrogen receptor alpha (ERα), with an IC50 value of 4.1 nM, indicating its high affinity for this receptor. Its mechanism of action involves binding to the ERα, preventing estrogen from activating the receptor, and promoting the degradation of the receptor itself. This dual action makes it effective in treating ER-positive breast cancers that depend on estrogen for growth and survival.
Unlike its parent compound fulvestrant, which requires intramuscular injection due to its poor oral bioavailability, ZB716 has been modified to be less susceptible to first-pass metabolism. This modification allows for oral administration, a significant advantage in terms of patient comfort and treatment adherence.
Related Terms
- Antiestrogen
- Orally active drug
- Estrogen receptor
- Metastatic breast cancer
- Selective estrogen receptor degrader
- Prodrug
- Fulvestrant
See Also
External links
- Medical encyclopedia article on ZB716
- Wikipedia's article - ZB716
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