Vepdegestrant - Cancer therapy drug
Prelims:
Science
& Technology, Biotechnology, Health
Mains:
GS
Paper II-Health, GS Paper III-Science & Technology
Current relevance:
Recently, U.S. Food and Drug
Administration (FDA) approved the drug vepdegestrant for patients with ESR1-mutated,
ER-positive, and HER2-negative advanced breast cancer. It is the
world’s first therapy that the FDA has approved that is based on PROTAC
technology.
Highlights:
1. Vepdegestrant is the world’s first therapy
that the U.S. Food and Drug Administration (FDA) has approved that is based on PROTAC
technology.
2.
PROTAC
(proteolysis-targeting chimaera):
i.
It
is a molecule-like substance which are designed to remove specific protien
from a cell.
ii.
This
is achieved with the help of bodily enzyme named “E3 Ligase”,
which is naturally involved in protein degradation process.
iii.
PROTAC
has two Ends, one side attaches to the target protein and other binds to E3
Ligase, by artificially bringing these together the PROTAC causes the target
protein to be degraded by the cell. This is called targeted
protein degradation.
3.
Advantages
over conventional Drugs:
i.
Conventional
drugs work by binding to a protein and blocking its function, often requiring
repeated doses. In contrast, PROTACs degrade the target protein
and are then released to destroy other proteins, allowing them to act
repeatedly like a catalyst.
ii.
PROTACs degrade the entire target
protein, thereby blocking all of its functions, unlike conventional
drugs that inhibit only a specific activity of the protein.
4.
Key
Features:
i.
Convenient
Oral Dosing: Intaken
as oral tablet, replacing the need for monthly intramuscular injections
required with therapies like fulvestrant.
ii. Manageable Safety Profile: Most side effects were mild, including fatigue, nausea, muscle pain, and temporary changes in liver enzymes or ECG findings.
Source: THE
HINDU - https://www.thehindu.com/sci-tech/science/why-fda-approval-for-vepdegestrant-is-a-major-shift-in-cancer-therapy/article71188088.ece