BET inhibitor - Pipeline Insight, 2024

This “BET inhibitor - Pipeline Insight, 2024” report provides comprehensive insights about 20+ companies and 20+ pipeline drugs in BET inhibitor pipeline landscape. It covers the pipeline drug profiles, including clinical and nonclinical stage products. It also covers the therapeutics assessment by product type, stage, route of administration, and molecule type. It further highlights the inactive pipeline products in this space.

Geography Covered

• Global coverage

BET inhibitor Understanding

BET inhibitor: Overview

Bromodomain and extraterminal domain (BET) proteins are epigenetic molecules that regulate the expression of multiple genes involved in carcinogenesis. The advent of potent inhibitors of BET proteins (BETi), which target either one or both bromodomains, represents an important step towards the goal of suppressing oncogenic networks within tumours.

BET-family members influence cell cycle progression by activating oncogenes such as MYC, JUNB, CCND1 and CCNA1. Consistent with a role in regulating the expression of cell cycle genes, knockdown of BRD4 leads to arrest in S phase in some cell types.17 BET proteins may directly activate oncogene transcription through recruitment to hyper-acetylated regulatory regions, as is seen is the regions surrounding MYC and CCNA1 genes. Upon being recruited to chromatin, BET-family members engage the mediator complex, which in turn, interacts with the core transcription machinery. Mediator provides a platform for the association of the p TEFb complex, leading to the phosphorylation of RNA POL II on serine 2, acting as a catalyst for transcriptionalelongation.

Development of BET inhibitors that disrupt BET protein binding to acetylated lysine residues of chromatin and suppress transcription of various oncogenes has shown promising results in breast cancer cells and xenograft models. Overall, BET inhibitors constitute a promising field of clinical search in hematologic malignancies and solid tumors. Breast cancer heterogeneity creates a therapeutic challenge that needs to be addressed by new therapeutic options. Results from ongoing studies remain to prove if BET inhibition can serve this purpose.

Report Highlights

The companies and academics are working to assess challenges and seek opportunities that could influence BET inhibitor R&D. The therapies under development are focused on novel approaches for BET inhibitor.

BET inhibitor Emerging Drugs Chapters

This segment of the BET inhibitor report encloses its detailed analysis of various drugs in different stages of clinical development, including phase III, II, I, preclinical and Discovery. It also helps to understand clinical trial details, expressive pharmacological action, agreements and collaborations, and the latest news and press releases.

BET inhibitor Emerging Drugs

Pelabresib: Constellation Pharmaceuticals Pelabresib, also known as CPI-0610, is a potent and selective small molecule designed to promote anti-tumor activity by selectively inhibiting the function of BET proteins to decrease the expression of abnormally expressed genes in cancer. The compound has demonstrated a wide therapeutic window, with activity seen at a 48 mg dose in a lymphoma study and with a maximum tolerated dose of 225 mg.

It is currently in phase III stage of development for the treatment of Myelofibrosis and is being developed by Constellation Pharmaceuticals.

Apabetalone: Resverlogix Apabetalone is an entirely new epigenetic therapeutic, taken orally to improve the condition of people suffering from vascular diseases by lowering the expression of disease-related genes. Expression of these genes promotes disease progression in patients suffering from vascular disease and diabetes, damaging arteries and increasing their risk of heart attacks and strokes. Apabetalone has a unique mechanism of action, working at the level of “transcription”. As a selective inhibitor of the BET family of proteins, apabetalone has the ability to normalize dysregulated epigenetics that lie at the heart of many chronicdiseases.

It is currently in phase III stage of development is being developed by Resverlogix.

BET inhibitor: Therapeutic Assessment

This segment of the report provides insights about the different BET inhibitor drugs segregated based on following parameters that define the scope of the report, such as:

Major Players working on BET inhibitor

There are approx. 20+ key companies which are developing the BET inhibitor. The companies which have their BET inhibitor drug candidates in the most advanced stage, i.e. Phase III include, Constellation Pharmaceuticals.

Phases

This report covers around 20+ products under different phases of clinical development like

• Late-stage products (Phase III)
• Mid-stage products (Phase II)
• Early-stage products (Phase I/II and Phase I) along with the details of
• Pre-clinical and Discovery stage candidates
• Discontinued & Inactive candidates

Route of Administration

BET inhibitor pipeline report provides the therapeutic assessment of the pipeline drugs by the Route of Administration. Products have been categorized under various ROAs such as

• Infusion
• Intradermal
• Intramuscular
• Intranasal
• Intravaginal
• Oral
• Parenteral
• Subcutaneous
• Topical

Molecule Type

Products have been categorized under various Molecule types such as

• Vaccines
• Monoclonal Antibody
• Peptides
• Polymer
• Small molecule

Product Type

Drugs have been categorized under various product types like Mono, Combination and Mono/Combination.

BET inhibitor: Pipeline Development Activities

The report provides insights into different therapeutic candidates in phase III, II, I, preclinical and discovery stage. It also analyses BET inhibitor therapeutic drugs key players involved in developing key drugs.

Pipeline Development Activities

The report covers the detailed information of collaborations, acquisition and merger, licensing along with a thorough therapeutic assessment of emerging BET inhibitor drugs.

BET inhibitor Report Insights

• BET inhibitor Pipeline Analysis
• Therapeutic Assessment
• Unmet Needs
• Impact of Drugs

BET inhibitor Report Assessment

• Pipeline Product Profiles
• Therapeutic Assessment
• Pipeline Assessment
• Inactive drugs assessment
• Unmet Needs

Key Questions

Current Scenario and Emerging Therapies:

• How many companies are developing BET inhibitor drugs?
• How many BET inhibitor drugs are developed by each company?
• How many emerging drugs are in mid-stage, and late-stage of development for BET inhibitor?
• What are the key collaborations (Industry-Industry, Industry-Academia), Mergers and acquisitions, licensing activities related to the BET inhibitor therapeutics?
• What are the recent trends, drug types and novel technologies developed to overcome the limitation of existing therapies?
• What are the clinical studies going on for BET inhibitor and their status?
• What are the key designations that have been granted to the emerging drugs?

Key Players

• Resverlogix
• Constellation Pharmaceuticals
• Zenith Epigenetics
• AbbVie
• Bristol-Myers Squibb
• Daiichi Sankyo Company
• Nuvation Bio
• TG therapeutics

Key Products

• Apabetalone
• Pelabresib
• ZEN-3694
• ABBV-744
• CC-95775
• PLX-2853
• NUV-868
• TG-1601
• BMS-986158

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