Product Description
An orally available inhibitor of mutant form of the isocitrate dehydrogenase type 1 (IDH1; IDH-1; IDH1 [NADP+] soluble), including the substitution mutation at arginine (R) in position 132, IDH1(R132), with potential antineoplastic activity. Upon oral administration, IDH1 mutant inhibitor LY3410738 specifically and covalently binds to and modifies a single cysteine (Cys269) in the allosteric binding pocket of mutant forms of IDH1, thereby inactivating IDH1. This inhibits the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This depletes 2-HG levels, prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing mutant forms of IDH1. In addition, LY3410738 has the ability to cross the blood-brain barrier (BBB). IDH1 mutations, including IDH1(R132) mutations, are highly expressed in certain malignancies, including gliomas; they initiate and drive cancer growth by both blocking cell differentiation and catalyzing the formation of 2HG. (Sourced from: https://www.cancer.gov/publications/dictionaries/cancer-drug/def/idh1-mutant-inhibitor-ly3410738)
Mechanisms of Action: IDH Inhibitor
Novel Mechanism: No
Modality: Small Molecule
Route of Administration: Oral
FDA Designation: None *
Approval Status: Not Approved
Approved Countries: None
Approved Indications: None
Known Adverse Events: None
Company: Eli Lilly
Company Location: INDIANAPOLIS IN 46285
Company CEO: David A. Ricks
Additonal Commercial Interests: None
Clinical Description
![Map of Global Clinical Trials for LY-3410738](https://pryzm-maps.s3.us-west-2.amazonaws.com/3945current_maps.png)
Countries in Clinic: Australia, Belgium, Canada, Finland, France, Germany, Hong Kong, Israel, Japan, Korea, Singapore, South Korea, Spain, Taiwan, United States
Active Clinical Trial Count: 5
Highest Development Phases
Phase 1: Acute Monocytic Leukemia|Acute Myeloid Leukemia|Acute Myelomonocytic Leukemia|Cholangiocarcinoma|Chondrosarcoma|Chronic Myeloid Leukemia|Chronic Myelomonocytic Leukemia|Glioma|Healthy Volunteers|Juvenile Myelomonocytic Leukemia,|Myelodysplastic Syndrome|Myeloproliferative Disorders|Preleukemia
Trial |
Phase |
Trial Status |
Disease |
Primary Completion Date |
Probability of Success |
---|---|---|---|---|---|
LOXO-IDH-20002 | P1 |
Active, not recruiting |
Cholangiocarcinoma|Chondrosarcoma|Glioma |
2023-07-17 |
|
LOXO-IDH-20001 | P1 |
Active, not recruiting |
Acute Monocytic Leukemia|Myelodysplastic Syndrome|Chronic Myeloid Leukemia|Preleukemia|Acute Myeloid Leukemia|Myeloproliferative Disorders|Chronic Myelomonocytic Leukemia|Acute Myelomonocytic Leukemia|Juvenile Myelomonocytic Leukemia, |
2023-07-03 |
|
LOXO-IDH-21004 | P1 |
Completed |
Healthy Volunteers |
2022-04-28 |
|
LOXO-IDH-20003 | P1 |
Completed |
Healthy Volunteers |
2021-08-04 |