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Lysine Specific Demethylase 1 (LSD-1) Inhibitors - Pipeline Insight, 2021

Lysine Specific Demethylase 1 (LSD-1) Inhibitors - Pipeline Insight, 2021

  • July 2021
  • 111 pages
  • ID: 6124425
  • Format: PDF
  • Delve Insight


Table of Contents

“Lysine Specific Demethylase 1 (LSD-1) Inhibitors - Pipeline Insight, 2021,” report provides comprehensive insights about 15+ companies and 15+ pipeline drugs in Lysine Specific Demethylase 1 (LSD-1) Inhibitors 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

Lysine Specific Demethylase 1 (LSD-1) Inhibitors Understanding

Lysine Specific Demethylase 1 (LSD-1) Inhibitors: Overview
Lysine specific demethylase 1 (LSD1, also known as KDM1A (lysine-specific demethylase 1A) or AOF2 (flavin-containing amine oxidase domain-containing protein 2), is an 852 amino acid, 110?kDa, flavin-dependent monoamine oxidase (MAO) protein. LSD1 has three structural domains that regulate its enzymatic activity and binding to several proteins. LSD1 contain a FAD-binding motif (FAD), the SWI3/Rac8/Moira (SWIRM) domain and a catalytic AOD domain.
Function - LSD1 is a central regulator of multiple relevant processes of cellular life, important either for general homeostasis or (if deregulated) tumor progression. LSD1 plays role in: Stem cell renewal, Cell proliferation and differentiation, Tumor progression, and Epithelial-mesenchymal transition. Its function in the nervous system has been recently expanded with the discovery of a new neuron-specific alternative splicing variant named neuroLSD1.
Lysine Specific Demethylase 1 (LSD-1) Inhibitors - Several LSD1 inhibitors including natural products, peptides, and synthetic compounds are currently undergoing clinical assessment for anticancer efficacy, especially in small lung cancer cells and acute myeloid leukemia. Pharmacological inhibition of LSD1 for cancer therapy can be into five subcategories: MAO inactivators and their derivatives, Natural products, Peptide inhibitors, Polyamine-based inhibitors, and Metal-based inhibitors.

Lysine Specific Demethylase 1 (LSD-1) Inhibitors Emerging Drugs Chapters
This segment of the Lysine Specific Demethylase 1 (LSD-1) Inhibitors 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.

Lysine Specific Demethylase 1 (LSD-1) Inhibitors Emerging Drugs
• IMG-7289: Imago BioSciences
IMG-7289 (Bomedemstat) is an orally available small molecule, discovered and developed by Imago BioSciences that inhibits lysine-specific demethylase 1 (LSD1 or KDM1A), an enzyme shown to be vital in cancer stem/progenitor cells, particularly neoplastic bone marrow cells. In non-clinical studies, bomedemstat demonstrated robust in vivo anti-tumor efficacy across a range of myeloid malignancies as a single agent and in combination with other therapeutic agents. The drug is being evaluated in Phase II clinical trial to treat patients with Essential thrombocythaemia, Myelofibrosis, and Polycythaemia Vera. In April 2021, the US Food and Drug Administration (FDA) has granted Fast Track designation for the development of IMG-7289 (bomedemstat) for the treatment of Essential Thrombocythemia. The drug has also been granted orphan drug designation by US FDA.
• Iadademstat: Oryzon Genomics
Iadademstat (ORY-1001) is a small oral molecule, which acts as a highly selective inhibitor of the epigenetic enzyme LSD1 and has a powerful differentiating effect in hematologic cancers. Beyond hematological cancers, the inhibition of LSD1 has been proposed as a valid therapeutic approach in some solid tumors such as small cell lung cancer (SCLC), neuroendocrine tumors, medulloblastoma and others. Iadademstat has been tested in four clinical trials (two in monotherapy in SCLC and AML, and two in combination, in SCLC and AML) in more than 100 patients.
• INCB059872: Incyte Corporation
INCB059872 is an orally available inhibitor of lysine-specific demethylase 1 (LSD1; lysine-specific histone demethylase 1A; KDM1A), with potential antineoplastic activity. Upon administration, INCB059872 binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4, respectively, through amine oxidation. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor-suppressor genes. A Phase I/II clinical trial is investigating INCN059872 to treat patients with Solid Tumors and Hematologic Malignancy.
• TAS1440: Astex Pharmaceuticals
TAS1440 is a Lysine-Specific Histone Demethylase 1 inhibitor (LSD1 [also named KDM1A]). LSD1 is an epigenetic regulator. It is aberrantly expressed in many cancers, including AML, where it impedes cellular differentiation which may contribute to leukemia development, cancer cell proliferation, cell metastasis, and invasiveness, and is associated with inferior prognosis. TAS1440 is being evaluated in a first-in-human Phase I clinical study in patients with relapsed/refractory AML.
• RASP-201: Rasna Therapeutics
RASP-201 is a novel, orally dosed, selective reversible inhibitor of lysine specific demethylase, or LSD1, a pathway that blocks differentiation and confers a poor prognosis to AML. RASP-201 when dosed orally shows in vivo therapeutic utility in murine (mouse) models of AML.
Further product details are provided in the report……..

Lysine Specific Demethylase 1 (LSD-1) Inhibitors: Therapeutic Assessment
This segment of the report provides insights about the different Lysine Specific Demethylase 1 (LSD-1) Inhibitors drugs segregated based on following parameters that define the scope of the report, such as:
• Major Players working on Lysine Specific Demethylase 1 (LSD-1) Inhibitors
There are approx. 15+ key companies which are developing the Lysine Specific Demethylase 1 (LSD-1) Inhibitors. The companies which have their Lysine Specific Demethylase 1 (LSD-1) Inhibitors drug candidates in the most advanced stage, i.e. phase II include, Imago BioSciences.
• Phases
This report covers around 15+ products under different phases of clinical development like
• Late-stage products (Phase III and
• Mid-stage products (Phase II and
• 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
Lysine Specific Demethylase 1 (LSD-1) Inhibitors pipeline report provides the therapeutic assessment of the pipeline drugs by the Route of Administration. Products have been categorized under various ROAs such as
• Intramuscular
• Oral
• Parenteral
• Subcutaneous
• Topical.
• Molecule Type

Products have been categorized under various Molecule types such as
• Small molecule
• Stem cell therapy
• Peptide
• Product Type
Drugs have been categorized under various product types like Mono, Combination and Mono/Combination.

Lysine Specific Demethylase 1 (LSD-1) Inhibitors: Pipeline Development Activities
The report provides insights into different therapeutic candidates in phase II, I, preclinical and discovery stage. It also analyses Lysine Specific Demethylase 1 (LSD-1) Inhibitors 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 Lysine Specific Demethylase 1 (LSD-1) Inhibitors drugs.

Report Highlights
• The companies and academics are working to assess challenges and seek opportunities that could influence Lysine Specific Demethylase 1 (LSD-1) Inhibitors R&D. The therapies under development are focused on novel approaches for Lysine Specific Demethylase 1 (LSD-1) Inhibitors.

Lysine Specific Demethylase 1 (LSD-1) Inhibitors Report Insights
• Lysine Specific Demethylase 1 (LSD-1) Inhibitors Pipeline Analysis

• Therapeutic Assessment
• Unmet Needs
• Impact of Drugs

Lysine Specific Demethylase 1 (LSD-1) Inhibitors 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 Lysine Specific Demethylase 1 (LSD-1) Inhibitors drugs?
• How many Lysine Specific Demethylase 1 (LSD-1) Inhibitors drugs are developed by each company?
• How many emerging drugs are in mid-stage, and late-stage of development for Lysine Specific Demethylase 1 (LSD-1) Inhibitors?
• What are the key collaborations (Industry–Industry, Industry–Academia), Mergers and acquisitions, licensing activities related to the Lysine Specific Demethylase 1 (LSD-1) Inhibitors 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 Lysine Specific Demethylase 1 (LSD-1) Inhibitors and their status?
• What are the key designations that have been granted to the emerging drugs?

Key Players
• Imago BioSciences
• Oryzon Genomics
• Celgene
• 4SC
• ExCellThera
• Incyte Corporation
• Salarius Pharmaceuticals
• Astex Pharmaceuticals
• CSPC ZhongQi Pharmaceutical
• Takeda
• Rasna Therapeutics
• Hanmi Pharmaceutical
• Constellation Therapeutics
• Salarius Pharmaceuticals

Key Products
• IMG-7289
• Ladademstat
• Vafidemstat
• CC-90011
• Domatinostat
• UM171
• INCB059872
• Seclidemstat
• TAS1440
• SYHA1807
• TAK-418
• HM97211
• CPI-482
• SP2509

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