CDK12 Inhibitor - Pipeline Insight, 2024

This “CDK12 Inhibitor- Pipeline Insight, 2024” report provides comprehensive insights about 3+ companies and 3+ pipeline drugs in CDK12 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

CDK12 Inhibitor: Understanding

CDK12 Inhibitor: Overview

Cyclin-dependent kinase 12 (CDK12) is one of the 20 members of cyclin-dependent kinases (CDK). Each of CDKs binds with cyclin play important roles in the control of cell cycle and cell division and regulates transcription in response to various cellular processes. As a transcription associated CDK, CDK12 binds with cyclin K phosphorylate RNA Pol II at CTD promoting transcription elongation. CDK12 can also interact with RNA processing factors to regulate RNA splicing. Furthermore, CDK12 mediated phosphorylation of RNA Pol II couples m RNA 3' end processing to participate in transcription termination. Besides, CDK12 plays critical role in regulating intronic polyadenylation, epigenetics, as well as translation. CDK12 alterations were found in different humancancers.

CDK12 is mainly composed of three domains: a central Cdc2-related protein kinase domain (KD), an N-terminal “arm”, about 700 amino acids, and a C-terminal “arm”, about 500 amino acids. The central KD is composed of 300 amino acids and is located at the center of CDK12. Its main function is to mediate the phosphorylation of the C-terminal domain (CTD) of RNAP II. There are 21 RS motifs in the first 400 amino acids of CDK12, and only one RS motif in the rest of the approximately 1000 amino acids. The RS domain, which is enriched arginine and serine, is considered as a prominent feature of CDK12. It was originally found in pre-messenger RNA (pre-m RNA) splicing factors that were important for spliceosome assembly and alternative splice-siteselection.

In CDK12, the RS domain mainly functions to target CDK12 to the nuclear speckles. The central KD and the RS domain endow CDK12 the capacity to directly link transcription with the splicing machinery. Proline-rich motifs (PRM) are located between the RS domain and the central KD and are also found in the C-terminal region. The PRM contains the consensus binding sites for Src homology 3 (SH3) and tryptophan (WW) regions which can mediate protein-protein interactions by binding proline-rich modules in ligands. The presence of the RS domain and PRM domain indicates that CDK12 is likely to take part in numerous protein-protein interactions. Notably, the closest human homologue of CDK12 is CDK13. While their sequences of KD are highly homologous, their C- and N-terminal regions differ between CDK12 and CDK13.

CDK12 plays an important role in promoting cancer cell growth, especially in cancers driven by dysregulated transcription factors, such as cancers dependent on MYC (neuroblastoma) and the EWS-FLI1 fusion oncoprotein (Ewing sarcoma). Neuroblastoma is a cancer highly dependent on transcriptional programs. MYC is a proto-oncogene and a major driver of many human cancers. Amplification of n-MYC (MYCN) leads to neuroblastoma. Studies have indicated that THZ1, a CDK12 inhibitor, inhibits MYC expression and tumor growth. In addition, CDK12 plays an important role in the processing of MYC precursor m RNA. Ewing sarcoma is characterized by chromosome rearrangement which fuses the strong transactivation domain of EWS protein with the DNA binding domain of FLI1 protein. EWS/FLI acts as both a transcriptional activator and a transcriptional repressor. Currently, treatment of Ewing sarcoma mainly uses CDK12 inhibitors THZ1 and THZ531, which impair DNA damage repair in an EWS/FLI-dependent manner. The combination of CDK12 and PARP inhibitors is highly active in Ewing Sarcoma. Taken together, targeting CDK12 may be a viable treatment strategy for cancers driven by dysregulated transcriptionfactors.

CDK12 Inhibitor- Pipeline Insight, 2024 report outlays comprehensive insights of present scenario and growth prospects across the indication. A detailed picture of the CDK12 Inhibitor pipeline landscape is provided which includes the disease overview and CDK12 Inhibitor treatment guidelines. The assessment part of the report embraces, in depth CDK12 Inhibitor commercial assessment and clinical assessment of the pipeline products under development. In the report, detailed description of the drug is given which includes mechanism of action of the drug, clinical studies, NDA approvals (if any), and product development activities comprising the technology, CDK12 Inhibitor collaborations, licensing, mergers and acquisition, funding, designations and other product related details.

Report Highlights

The companies and academics are working to assess challenges and seek opportunities that could influence CDK12 Inhibitor R&D. The therapies under development are focused on novel approaches to treat/improve CDK12 Inhibitor.

CDK12 Inhibitor Emerging Drugs Chapters

This segment of the CDK12 Inhibitor report encloses its detailed analysis of various drugs in different stages of clinical development, including phase 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.

CDK12 Inhibitor Emerging Drugs

CT7439: Carrick Therapeutics CT7439 is an inhibitor of CDK12/13 as well as a 'glue degrader' of Cyclin-K, which is the obligate co-factor for CDK12/13, giving both first-in-class and best-in-class potential. This dual modality significantly increases the potency of the compound and leads to the inhibition of DNA repair at the transcriptional level. CDK12/13 regulates gene transcription through the activation of RNA Polymerase II. It has the potential to synergise with other agents targeting DDR such as the PARP inhibitors in multiple cancer types including breast, ovarian and Ewing’s Sarcoma. The Company plans to initiate the Phase I clinical trial in the first half of 2024 and intends to enroll patients with advanced solid tumors, including breast, ovarian and Ewing's Sarcoma.

OKI 1546: On Kure Therapeutics OKI-1546 is a novel, covalent inhibitor of CDK12 and CDK13 that is potent, specific, orally available, and shows in vivo target engagement and tumor growth inhibition in preclinical cancer models. OKI-1546 showed activity in vivo as a single agent and cellular data suggest that inhibition of CDK12 has the potential to enhance the effects of other DDR-targeting therapeuticagents.

CDK12 Inhibitor: Therapeutic Assessment

This segment of the report provides insights about the different CDK12 Inhibitor drugs segregated based on following parameters that define the scope of the report, such as:

Major Players in CDK12 Inhibitor

• There are approx. 3+ key companies which are developing the therapies for CDK12 Inhibitor. The companies which have their CDK12 Inhibitor drug candidates in the most advanced stage, i.e. IND Stage include, Carrick Therapeutics.

Phases

This report covers around 3+ products under different phases of clinical development like

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

Route of Administration

CDK12 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

• Oral
• Intravenous
• Subcutaneous
• Parenteral
• Topical

Molecule Type

Products have been categorized under various Molecule types such as

• Recombinant fusion proteins
• Small molecule
• Monoclonal antibody
• Peptide
• Polymer
• Gene therapy

Product Type

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

CDK12 Inhibitor: Pipeline Development Activities

The report provides insights into different therapeutic candidates in phase II, I, preclinical and discovery stage. It also analyses CDK12 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 CDK12 Inhibitor drugs.

CDK12 Inhibitor Report Insights

• CDK12 Inhibitor Pipeline Analysis
• Therapeutic Assessment
• Unmet Needs
• Impact of Drugs

CDK12 Inhibitor Report Assessment

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

Key Questions

Current Treatment Scenario and Emerging Therapies:

• How many companies are developing CDK12 Inhibitor drugs?
• How many CDK12 Inhibitor drugs are developed by each company?
• How many emerging drugs are in mid-stage, and late-stage of development for the treatment of CDK12 Inhibitor?
• What are the key collaborations (Industry-Industry, Industry-Academia), Mergers and acquisitions, licensing activities related to the CDK12 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 CDK12 Inhibitor and their status?
• What are the key designations that have been granted to the emerging drugs?

Key Players

• Carrick Therapeutics
• On KureTherapeutics

Key Products

• CT7439
• OKI-1546

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