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Overview

Tags

Neoplasms

Immune System Diseases

Endocrinology and Metabolic Disease

Recombinant polypeptide

Synthetic peptide

Small molecule drug

Disease domain score

A glimpse into the focused therapeutic areas

Technology Platform

Most used technologies in drug development

Targets

Most frequently developed targets

Disease Domain	Count

Neoplasms	2
Endocrinology and Metabolic Disease	1
Infectious Diseases	1
Immune System Diseases	1

Top 5 Drug Type	Count

Recombinant polypeptide	3
Synthetic peptide	1
Small molecule drug	1

Top 5 Target	Count

GCGR x GLP-1R	1
CDK(Cyclin-dependent kinase)	1

AbstractA series of coumarin and 1‐Aza coumarin analogues of miconazole(5 a‐6 e) were synthesized from 2‐bromo‐1‐(2,4‐dichlorophenyl)ethanone and diversification was achieved by synthesizing coumarin‐benzimidazole(7 a‐7 e) and 1‐aza coumarin‐benzimidazole(8 a‐8 e) hybrids of miconazole and evaluated for in‐vitro anti‐microbial activities. Among the tested compounds, 8 b‐8 e were found to be effective as anti‐fungal against C. albicans, C. utilis and C. krusei, with activity compared to that of the standard. Comparative docking studies with mevalonate‐5‐diphosphatedecarboxylase shows better binding affinity than imidazole counterparts which is primarily attributed to extended π‐alkyl interactions facilitated by benzimidazole.

01 Aug 2017·Cancer Chemotherapy and PharmacologyQ4 · MEDICINE

Human microdosing and mice xenograft data of AGM-130 applied to estimate efficacious doses in patients

Q4 · MEDICINE

Article

Author: Ban, Sooho ; Kim, Seon-Myung ; Yim, Dong-Seok ; Shin, Young G ; Park, Gab-Jin ; Kim, Hyung Sik ; Park, Moon-Young ; Kim, San-Ho ; Park, Wan-Su ; Kim, Yong-Chul ; Han, Seunghoon

PURPOSEAGM-130 is a cyclin-dependent kinase inhibitor that exhibits dose-dependent efficacy in xenograft mouse models. During preclinical pharmacokinetic (PK) studies, mice and rats showed comparable PK parameters while dogs showed unusually high clearance (CL), which has made human PK prediction challenging. To address this discrepancy, we performed a human microdosing PK and developed a mouse PK/PD model in order to guide the first-in-human studies.METHODSA microdose of AGM-130 was given via intravenous injection to healthy subjects. Efficacy data obtained using MCF-7 breast cancer cells implanted in mice was analyzed using pre-existing tumor growth inhibition models. We simulated a human PK/PD profile with the PK parameters obtained from the microdose study and the PD parameters estimated from the xenograft PK/PD model.RESULTSThe human CL of AGM-130 was 3.08 L/h/kg, which was comparable to CL in mice and rats. The time-courses of tumor growth in xenograft model was well described by a preexisting model. Our simulation indicated that the human doses needed for 50 and 90% inhibition of tumor growth were about 100 and 400 mg, respectively.CONCLUSIONSThis is the first report of using microdose PK and xenograft PK/PD model to predict efficacious doses before the first-in-human trial in cancer patients. In addition, this work highlights the importance of integration of all of information in PK/PD analysis and illustrates how modeling and simulation can be used to add value in the early stages of drug development.

100 Deals associated with ANYGEN Co., Ltd.

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100 Translational Medicine associated with ANYGEN Co., Ltd.

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Pipeline

Pipeline Snapshot as of 19 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

Preclinical

4

1

Phase 1 Clinical

Other

3

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

AGM-130 ( CDK )	Triple Negative Breast Cancer More	Phase 1
AGM-217 ( GCGR x GLP-1R )	Obesity More	Preclinical
AGM-260	Colitis, Ulcerative More	Preclinical
AGM-380	COVID-19 More	Preclinical
AGM-331	Neoplasms More	Preclinical