Liver Disease

ID119031166

• A potent non-steroidal FXR agonist to treat NASH:
 - Mechanism of action that inhibits the synthesis of bile acid
 - Strong activity and selectivity demonstrated in nonclinical studies
 - Significantly reduced NAFLD Activity score and fibrosis in animal models of NASH
 - Regulated direct FXR target genes in a dose-dependent manner in vivo
 - Not importantly altered plasma level of ALT/AST and LDL-C at the effective dose
• Phase 1 has started in US in October to evaluate safety and pharmacokinetics
 - Phase I Single Assending dose study in Progress

NASH : NonAlcoholic SteatoHepatitis, NAFLD : NonAlcoholic Fatty Liver Disease,
FXR : Farnesoid X Receptor, ALT : Alanine aminotransferase,
AST : Aspartate aminotransferase, LDL-C : Low-Density Lipoprotein Cholesterol

Liver Disease

ID119050134

• A potent ATX inhibitors for Liver cirrhosis treatment
• ID119050134 inhibits the production of LPA by ATX and inhibits the differentiation of Hepatic Stellate Cell (HSC) into Myofibroblast with strong fibrogenic activity
• Phase 1 IND submission is planned in 2024

ATX: Autotaxin LPA: Lysophosphatidic acid HSC: Hepatic stellate cell

CNS

LASMIDITAN

• Migraine therapy with an innovative mechanism of action with no restrictions on use in
    cardiovascular disease patients
 - The first and only Ditan drug approved by the FDA with a different mechanism from triptans
    (serotonin 1B receptor agonists) and NSAIDs, which have been used as migraine treatments.
 - Overcoming the limitations of existing triptans (limited use in cardiovascular patients) by
     exhibiting 470-fold or more affinity for serotonin 1F receptors compared to serotonin 1B and
     1D receptors associated with vasoconstriction
• NDA approval by MFDS on May 2022

NSAIDs : Non-steroidal anti-inflammatory drugs

CNS

ID119040338

• A Novel Non-dopaminergic treatment for Parkinson’s disease
  - First-In-Class Adenosine A1/A2A Dual Receptor Antagonist
  - Exceptional drug absorption and excellent BBB (Blood-Brain Barrier) permeability
  - (ID119040338) Demonstrated superior efficacy in long-term duration and in behavioral improvement(or motor and non-motor symptoms) compared to other drugs in MPTP-monkey models.
  - Expected to improve non-motor symptoms in Parkinson’s disease through Adenosine A1/A2a Dual Receptor Antagonism
• IND Application expected in 2024

Metabolic Disease

IDG16177

• A GPR40 agonist to treat type 2 diabetes mellitus
 - High oral absolute bioavailability in pre-clinical species
 - A defined MoA, activating β-arrestin2 recruitment as well as Gq-dependent pathway
 - Glucose-dependent insulin secretion & free of hypoglycemic risk
 - Superior to fasiglifam in glucose reduction in normal and diabetic rat studies
 - Potentially no risk of DILI (drug-induced liver injury)
• Phase 1 has started in Germany in July 2021 to evaluate safety and pharmacokinetics
    (NCT04982705)
• Phase 1 (SAD, MAD) completed in August 2022
• Phase 1 patient dosing protocol submitted by BfArM in Oct 2022
• Phase I clinical trials for patients was administered in January 2023.
• Completed recruitment of subjects for Phase 1 clinical trial in patients in May 2023

Metabolic Disease

ID110521156

•A small-molecule glucagon-like peptide (GLP)-1 receptor agonist to treat type 2 diabetes
 - Being developed as an oral drug
 - A defined MoA, increasing intra-cellular cAMP levels through the activation of Gα subunit pathway
 - No risk for hypoglycemic shock by glucose-dependent insulin secretion
 - Overcame the disadvantages of existing injection drugs (improved safety profile and
    patient adherence)
 - Potential of expansion to various indications including obesity and NASH
• Nonclinical studies and IND writing (CTD/IB) completion expected in Q1 2023
• IND submission expected in Q2 2023

GLP-1 : Glucagon-like peptide-1, NASH : NonAlcoholic SteatoHepatitis

Ophthalmology

IDB0062

• A dual-targeting antibody fragment drug for wet AMD
 - A dual target antibody fragment in which a tissue penetrating peptide targeting NRP1 is linked to the anti-VEGFA antibody fragment
 - Stronger efficacy by inhibition of multiple pathological growth factors in ocular angiogenic diseases(VEGF-A, -B, -C, PlGF2, PDGFBB)
  -Delay and suppression of subretinal fibrosis formation through macrophage regulation
 - Expected extended dosing interval based on improved ocular PK profile(Once every 2 or 3 months) 
 - Possibility on less invasive treatment through tissue-penetrating peptides
• Possibility of absence of ocular/systemic side effects through toxicological benefit​
• Manufacturing strain established with Global CDMO

Ophthalmology

ID110410395

• First-in-class small molecule CFTR activator/PDE4 inhibitor to treat dry eye disease
 - A novel mode of action in which DED symptoms are improved by restoration of tear film homeostasis through tear secretion and anti-inflammatory action.
 - targets to improve both signs and symptoms with favorable tolerability profile and
    simplified dosing
• IND submission expected in H2 2022

CFTR : Cystic Fibrosis Transmembrane Conductance Regulator

Gastrointestinal Disease

ID120040002

• A novel Potassium-Competitive Acid Blocker (P-CAB) to treat gastric acid related diseases:
 - Strong inhibition of proton pump (H+/K+ ATPase)
 - Long retention time in stomach for effective proton pump inhibition
 - Inhibition of basal gastric acid secretion and fast-onset of efficacy in vivo

• MFDS IND approval in Nov 2022 • Phase 1 Single Ascending Dose Completed. Multiple Ascending Dose in Progress

Respiratory Disease

ID119010023

• A nitric oxide-donating PDE5 inhibitor for ARDS, PAH
 - Highly selective and potent in vitro activity
 - Efficacy shown in an acute lung injury mouse model
• in vivo efficacy study, formulation, PK analysis are on-going
• IND submission expected in 1Q 2023

ARDS : Acute Respiratory Distress Syndrome, PDE5 : PhosphoDiEsterase 5