Vepdegestrant and PROTAC Technology for Cancer Treatment

#GS-3 #Science & Technology #Biotechnology #Health #Cancer Treatment #PROTAC Technology

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The U.S. Food and Drug Administration (FDA) recently approved vepdegestrant. This marks a major milestone because it is the world's first approved medicine using PROTAC technology.

Vepdegestrant is a new oral pill made with PROTAC technology. Instead of just blocking bad proteins like older medicines, it uses the cell's own cleanup system to destroy them completely.
Two pharmaceutical companies, Arvinas, Inc. and Pfizer, worked together to create this new therapy.
It treats advanced breast cancer that is ESR1-mutated, ER-positive, and HER2-negative. It targets mutated estrogen receptors that no longer respond to normal hormone treatments.

A PROTAC molecule has two active ends. One side grabs the target protein, while the other side connects to an E3 ligase enzyme.
By holding both pieces together at the same time, the molecule builds a temporary structure called a ternary complex.
Next, the E3 ligase attaches ubiquitin tags onto the bad protein. This marks the target protein for permanent destruction inside the cell.
A cellular machine called a proteasome breaks down the marked protein into amino acids. Meanwhile, the PROTAC molecule leaves untouched to attack more target proteins.

Traditional drugs only block protein signals, but vepdegestrant removes the estrogen receptor entirely. This stops all cancer growth signals coming from that protein.
One single molecule of vepdegestrant can destroy many target proteins repeatedly. This high efficiency means patients can take smaller doses.
Patients take this treatment as a once-daily oral tablet. It replaces painful monthly injection therapies like fulvestrant.
In a trial of 624 patients, vepdegestrant kept cancer from growing for a median of 5 months, compared to only 2.1 months with fulvestrant.
The drug causes mostly mild side effects such as fatigue, nausea, muscle aches, and short-term shifts in liver enzymes or heart rhythm readings.

PROTAC technology allows scientists to destroy protein targets that were once considered impossible to treat with conventional drugs.
By destroying mutated receptors instead of just blocking them, vepdegestrant offers new hope when standard hormone therapies stop working in advanced cancer.