Oscotec Inc.

Translating science into medicine
Sign Up
PRESS

New Drug Candidate

| Translating science into medicine


SYK inhibitor (SKI-O-703)


Indication

Rheumatoid arthritis

Unmet medical needs

Although MTX, small molecular drug, is the current gold-standard for treatment of rheumatoid arthritis, it is suffering from low efficacy, frequent cases of non-responsiiceness and a variety of adverse events, Biologics often exhibit reasonable efficacy, but high costs, limited administration routes(injection), immunogenicity and porential tumor formation are points of concern in using them, Also, many patients are non-responsive to biologics. Therefore, the key unmet needs for rheumatoid arthritis therapy are achievement of adequate therapeutic efficacy for RA patients who are non-responsive to DMARDs and Biologics, Management of adverse events to a lower level, and improvement in convenience via oral administration.

Target patient

Patient with rheumatoid arthritis who are non-responsive to MTX and biologics

Development status

SKI-O-703 is currently in phase IIa clinical trial in US, EU, and Korea.

Competitive drug

First-in-class SYK inhibitor for rheumatoid arthritis

Competitive advantages

Fostamatinib (R788, Rigel Pharmaceuticals, Inc) was discontinued after Phase III clinical trials due to low efficacy and severe adverse events which were caused from low selectivity. P505-15 (PRT062607, Portola harmaceuticals Inc) exhibited high selectivity, but revealed a high level of toxicity and low bioavailability.
SKI-O-703 demonstrated a superior selectivity to SYK, an improved bioavailability (BA 60%) and a low level of toxicity (ED50 1.4 mg/kg in animal with safety margin of over 80 folds)

SYK inhibitor (SKI-O-703)


Indications

Immune thrombocytopenia

Unmet medical needs

Treatments for patients with immune thrombocytopenia include corticosteroids, intravenous immunoglobulin (IVIG), anti-D, splenectomy, and rituximab. However, despite its treatments, there are quite a few patients with persistently low platelet counts. Therefore, the key unmet needs for immune thrombocytopenia therapy are achievement of adequate therapeutic efficacy.

Target patient

Patient with persistent and chronic ITP

Development stage

SKI-O-703 is currently in phase IIa clinical trial in US, EU, and Korea.

Competitive drug

R788 (Fostamatinib, Tavlesse)

Competitive advantages

R788 is the first small molecule SYK inhibitor and a prodrug of R406. R788 new drug application has been submitted to US Food and Drug Administration (FDA) for the treatment of patients with refractory ITP despite its marginal efficacy by off-target in clinical trials. SKI-O-703 displayed high selectivity and potency against SYK in both biochemical and cell-based assays. Selective SYK inhibition by SKI-O-592 prevents FcγR mediated phagocytosis in vitro and downregulates cluster of differentiation (CD) 63 expression on peripheral blood basophils in healthy adults.

FLT3 inhibitor (SKI-G-801)


Indication

Acute myeloid leukemia (AML)

Unmet needs

AML is a heterogeneous disease of the hematopoietic stem cells, and closely associated with age. Elderly AML paients ( > 60 yrs ) show low response and high relapse rate after first-line treatment, such as cytrabine and anthracycline. One of reason for the drug-resistance is known for aberrantly activating FLT3 mutations, which FLT3-ITD (internal tandom duplication) and FLT3-TKD (tyrosine kinase domain) mutations have been characterized in approximately 35% of AML pathology. Therefore, the most significant unmet need in AML is for more effective and toleravle therapies in elderly patents.

Target population

AML patients harboring FLT3 activating mutations (FLT3-ITD and FLT3-TKD)

Developmental stage

Approval of US FDA IND (2016). Phase I clinical study is on going in us 5 stires.

Competitive drugs

PCK412(Novartis), AC220(Daiichi Sankyo), ASP2215 (Astellas)

Competitive advantages

SKI-G-801 (HCI salt of G-749) is highly potent against clinically known FLT3 mutants harboring FLT3-F691L and FLT3-D835Y that confer resistance to PKC412 and AC220. Notably, G-749 retained its inhibitory potency in various drug-resistance milieus such as patient plasma and stromal protection. Furthermore, it displayed potent antileukemic activity in bone marrow blasts from AML patients regardless of FLT3 mutation status, including those with little or only minor responses to AC220 or PKC412. Intravenous administration of SKI-G-801 suppressed significant FLT3 pathway in tumor tissue, and yielded complete tumor regression and no tumor relapse in xenograft model without relapse in mouse xenograft model. Thus, SKI-G-801 appears to be a promising next generation drug candidate for the treatment of relapsed and refractory AML patients with various FLT3-ITD/FLT3-TKD mutants and further shows the ability to overcome drug resistance, Pharmacological results have been reported in Blood journal in 2014. Orphan drug designation obtained from us FDA in November 2018.

EGFR double mutation inhibitor (GNS-1480, YH25448)


Indications

Non-small cell lung cancer third-generation target

Unmet medical needs

EGFR-mutant derived non-small cell lung cancer patients account for 10-15% of all non-small cell lung cancer patients in Europe and 30-40% in Asia. These patients exhibited EGFR mutations at the time of diagnosis and progressed to T790 mutations in two of three patients with non-small cell lung cancer progressing after EGFR-TKI treatment. For patients with these mutations, therapies are currently limited. Therefore, the development of a third generation EGFR drug that can treat the T790M mutation is urgently required.

Target patient

Patients resistant to existing EGFR inhibitor drugs, iressa and tarceva.

Development stage

Lead compounds discovered by Oscotec were transferred to Yuhan corporation. Yuhan have finished non-clinical studies and filed IND for Phase I/II clinical studies and will star clinical trials in early 2017.

Competitive drug

Osimertinib (AstraZeneca), Olmutinib (Hanmi)

Competitive advantages

GNS-1480 has excellent drug efficacy against dual mutant non-small cell lung cacer resistant to the existing EGFR inhibitor drugs, iressa and tarceva. Because of its high blood-brain barrier permeability GNS-1480 is a potential candidate expected to have excellent effects for patients with brain metastatic non-small-cell lung cancer who do not have an effective treatment even at a high incidence rate.

© k2s0o1d6e0s8i2g7n. ALL RIGHTS RESERVED.
Requesting to the server, please wait.