On May 24, 2022 PeLeMed reported that it will present the preclinical study results of the FLT3/RET dual inhibitor candidate ‘PLM-102’ at the American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) 2022 (ASCO 2022) (Press release, PeLeMed, MAY 24, 2022, View Source [SID1234615603]).
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PLM-102, a target anticancer drug candidate of Pelemed, targets even FLT3-resistant mutations (D835Y, F691L) that develop resistance after treatment with existing drugs such as ‘Xospata, gilteritinib’, an FLT3 inhibitor for the treatment of acute myeloid leukemia (AML). do. Pelemed is aiming to submit an IND to the Korean and US Food and Drug Administration (FDA) next year.
At this ASCO (Free ASCO Whitepaper), Pelemed will present △in vitro biochemical, cellular △ in vitro efficacy, △mode of action, etc. of PLM-102 along with the existing drug Zosphata. .
Specifically, PLM-102 showed an excellent Kd value for binding even at a lower dose compared to the FLT3/AXL inhibitor Zosphata in the binding affinity test. The Kd value of PLM-102 was 0.019 nM (vs 1.4 nM) for normal FLT3 and 0.01 to 1.1 nM (vs 0.16 to 19 nM) for TKD mutant, which showed a lower Kd value than that of Zosphata.
Pelemed’s PLM-102 resulted in effective cell growth inhibition at a lower dose than Zosphata in acute myeloid leukemia cell lines (MV4-11, MOLM-13, MOLM-14) and Ba/F3 cell lines with FLT3 mutations. showed
A tumor mouse model administered with a dose of 5 mg/kg or more of PLM-102 showed complete remission with tumor growth inhibition when administered orally once a day. In addition, Pelemed explained that the anticancer effect was also confirmed in drug-resistant double mutation models (ITD/F691L, ITD/D835Y) administered with PLM-102.
Pelemed confirmed the RET inhibitory effect of PLM-102 and the decomposition effect of RET and FLT3 proteins. This proteolysis phenomenon did not appear in Zosphata and another approved RET inhibitor, Roche’s ‘Gavreto, pralsetinib’, indicating a differentiated mechanism of RLM-102, the company explained.
Acute myeloid leukemia (AML) is a type of blood cancer in which tumor cells appear in the blood or bone marrow. FLT3 mutations are observed in about 30% of acute myeloid leukemia patients. It is known that 50% of patients with acute myeloid leukemia who have achieved complete remission with high-intensity chemotherapy experience recurrence, and patients with FLT3 mutations are known to have a higher risk of recurrence and a lower survival rate than those who do not.
An official from Pelemed said, "PLM-102, which has a differentiated mechanism, is under non-clinical research this year.