【Product for Licensing】 A FIC TLR9 targeted ODN Immunomodulator for the Treatment of Allergic Diseases

项目ID：BP-20240522-OR-040

Product Brief Summary

• Product Name: A FIC TLR9 targeted ODN Immunomodulator
• Modality: Oligonucleotide DNA
• Target: TLR9
• MOA: Inhibition of Th2 or Th17 mediated inflammatory diseases
• Therapeutic Area: Allergic Diseases
• Current Stage: Phase I
• Rights Available: China/Global Right
• Collaboration Mode: License out

Key Allergic Disease Global Markets

Allergic rhinitis：Predicted to increase from $14.35 billions in 2022 to $18.02 billions in 2030

Atopic Dermatitis：Predicted to increase from $15.2 billions in 2021 to $28.7 billions in 2030 with the fastest growing market in Asia

Allergic asthma：Predicted to increase from $7.0 billions in 2021 to $8.87 billions in 2029

Chronic obstructive pulmonary diseases（COPD）：Predicted to increase from $18.1 billions in 2022 to $29.88 billions in 2032

Advantages

• First time such class of unmodified ODN entered clinical trial
• Strong IP position, high barrier for IP evasion
• Inhibition of early cascade of Th2 responses for the treatment of allergic diseases
• Direct competitor of allergic disease blockbuster drug Dupixent®
• Indications include allergic rhinitis, atopic dermatitis, allergic asthma, obstructive pulmonary diseases (COPD) and other eosinophilia related allergic diseases
• Local administration results in excellent safety, tolerability and compliances
• Cost of ODNs substantially lower than that of mAb

Current Progresses

• Nasal spray formulation for Seasonal Allergic Rhinitis (SAR) Phase I trial ongoing, CSR at the end of Oct. 2024
• SAR Phase II trial planed to start in March 2025
• Atopic dermatitis (AD) preclinical studies ongoing, China IND early next year
• Significant efficacy in AR in small scale IIT and volunteer uses
• Small scale use of product ointment for AD showed significant efficacy
• Allergic asthma and COPD preclinical studies in planning stage

Mechanism of Actions

1. Stimulates a type of innate immune cells to directly or indirectly produce large amount of type I/II/III interferons
2. Enhances Th1 immune response thus suppressing Th2 response
3. Induces IFNγ and IL-10 secreting Tr1 cells
4. Inhibits Th17 immune responses
5. Is a strong immunomodulator in inhibiting Th2 responses without stimulating Inflammatory cytokine releases

Comparison between this product and Dupixent®

Key Drug Properties

• Strong immunomodulating ODN with unique sequences and structures
• Unique formulation without unpleasant smell, no local irritation, excellent safety and tolerability
• DS stable at -20℃ >3 years; Nasal spray formulation stable at 2-8 ℃ for >2 years; room temperature for at least 1 year

Backgrounds and Differentiations

• This type of immunomodulating ODNs has been studied extensively in the preclinical stage with excellent efficacy in the treatment of allergic diseases including AR, allergic asthma and airway remodeling
• Due to the poor developability of such ODNs (easily form aggregates), clinical development has been hindered
• Three groups tried to overcome the developability issues with limited successes
• Thinking out of box has designed a series of ODNs with unique sequence combinations and structures, overcoming the developability issues
• This product is the most potent ODN with minimal aggregations and excellent developability in this innovative series
• The newly discovered rules governing the aggregations and potencies are novel

Phase I: SAD+MAD Progresses

A Double-blind and Randomized Single Center Phase 1 Dose Escalation Clinical Trial Evaluating Safety, Tolerability and PK/PD of Nasal Spray in Chinese Healthy Adult Population

Subjects：Male/Female healthy volunteers；

Sample numbers：SAD (=36 ) + MAD (n=16)，total 52；

100-400μg dose completed with excellent safety and tolerability; 800μg SAD and 400μg MAD ongoing

Evaluation in Safety/Tolerability and Efficacyin a Small IIT

• Well tolerated without any safety or tolerability issues
• Significant symptoms relieves in more severe patients

A Case of Atopic Dermatitis Patient with Ointment Treatment

~10 years AD on the forehead flares up frequently, requires frequent use of 1% hydrocortisone ointment treatment to relieve symptoms. Skin symptoms include extreme itchiness, redness, thinning and flaky; needs antibiotic ointment for skin infection. Significant improvement seen at 2 weeks after treatment; Not longer needs treatment at week 8

Comparison between this product and Current AR Drugs

Contact

• If interested, please contact DrugTimes BD Team at BD@drugtimes.cn. Many thanks!