Inhibition of BRD proteins suppresses the phenotype of uterine fibroids
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Publication Number
US-12533360-B2
Publication Date
2026-01-27
Expiration Date
Abstract
In aspects, the present disclosure provides a method of treating or preventing a uterine fibroid in a female mammal, the method comprising, consisting essentially of, or consisting of administering to the female mammal an effective amount of an inhibitor of bromodomain (BRD) protein.
Core Innovation
The disclosure describes treating or preventing uterine fibroids by administering an effective amount of a bromodomain (BRD) protein inhibitor to a female mammal, preferably a human. The approach is centered on inhibiting BRD proteins using a BRD protein inhibitor, and uterine fibroids are also referred to as uterine leiomyoma.
The disclosure specifies example BRD protein inhibitors including TP-472, I-BRD9, (+)-JQ1, I-BET762, and others. An Example describes that BRD2, BRD3, and BRD9 are elevated in human UF tissue versus myometrium, and includes comparison of cultured immortalized UF cells (HuLM) versus myometrium cells (UTSM) in the presence of BRD inhibitor treatment.
In cultured HuLM versus UTSM cells, BRD inhibitor treatment is described as suppressing an UF phenotype by reducing proliferation markers (PCNA) and fibronectin (FN). BRD9 inhibition is further described as increasing BCL-2, producing morphology changes, downregulating m6A regulators including YTHDC1, YTHDC2, YTHDF2, and METTL3, and altering transcription and bio-process pathways including E2F, MYC target, G2M checkpoint, and mitotic spindle.
Claims Coverage
The document includes one independent claim directed to treating a uterine fibroid and dependent claims that refine the BRD protein inhibitor and the treated subject. The claim set covers 5 inventive features.
Administering an effective amount of a BRD inhibitor to treat a uterine fibroid
A method of treating a uterine fibroid in a female mammal comprising administering to the female mammal an effective amount of an inhibitor of bromodomain protein (BRD).
Using a specific set of BRD inhibitors
The method uses an inhibitor of BRD selected from TP-472, I-BRD9, JQ1, or I-BET762.
Using TP-472 as the BRD inhibitor
The method uses TP-472 as the inhibitor of BRD.
Treating a human female mammal
The method is performed using a human female mammal.
Using I-BET762 as the BRD inhibitor
The method uses the BRD inhibitor I-BET762.
Overall claim coverage centers on treating uterine fibroids by administering an effective amount of an inhibitor of bromodomain protein (BRD), with refinements that specify particular named BRD inhibitors and optionally restrict the subject to a human female mammal.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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