Lasmotinib
CAS 2127107-15-5
MF C19H19FN4O2S MW386.4 g/mol
3-(carbamoylamino)-5-[2-(3-fluorophenyl)ethynyl]-N-[(3S)-piperidin-3-yl]thiophene-2-carboxamide
- N-(2-(N-((3S)(3-Piperidyl))carbamoyl)-5-(2-(3-fluorophenyl)ethynyl)(3-thienyl))aminamide
- 2-Thiophenecarboxamide, 3-((aminocarbonyl)amino)-5-(2-(3-fluorophenyl)ethynyl)-N-(3S)-3-piperidinyl-
- 3-(carbamoylamino)-5-[2-(3-fluorophenyl)ethynyl]-N-[(3S)-piperidin-3-yl]thiophene-2-carboxamide
- 2-Thiophenecarboxamide, 3-[(aminocarbonyl)amino]-5-[2-(3-fluorophenyl)ethynyl]-N-(3S)-3-piperidinyl-
- 3-(carbamoylamino)-5-(2-(3-fluorophenyl)ethynyl)-N-((3S)-piperidin-3-yl)thiophene-2-carboxamide
3-(carbamoylamino)-5-[(3-fluorophenyl)ethynyl]-N-[(3S)-piperidin-3-yl]thiophene-2-carboxamide
tyrosine kinase inhibitor, antineoplastic, PHI-101, PHI 101, U2UY9TBQ8Z
Lasmotinib (also known by its research code PHI-101) is a next-generation, orally bioavailable targeted cancer therapy. It functions as a dual FLT3 and CHK2 inhibitor. It is primarily being investigated to treat Acute Myeloid Leukemia (AML) and ovarian cancer.
How It Works
- FLT3 Inhibition: It targets FMS-like tyrosine kinase 3 (FLT3), an enzyme that is often mutated in AML. Lasmotinib is designed to attack not just single activating mutations (ITD or TKD), but also difficult-to-treat double and triple-resistant mutations.
- CHK2 Inhibition: It also inhibits Checkpoint Kinase 2 (CHK2), preventing cancer cells from repairing DNA damage. This causes the cancer cells to undergo apoptosis (programmed cell death).
Key Clinical Advantages
- High Efficacy: In relapsed or refractory AML patients who have previously failed other FLT3 inhibitors, lasmotinib has demonstrated high rates of composite complete remission.
- Safety Profile: Preclinical and early-stage trials indicate a promising safety profile with a very low or 0% occurrence rate of cardiotoxicity (heart damage), which is a common hurdle for some other FLT3-targeting drugs.
Current Development & Combinations
- Developer: Discovered by Seoul National University Hospital and being developed by Pharos iBio.
- Synergistic Therapies: Lasmotinib is currently moving into global clinical trials as a powerful combination therapy. Research shows it synergizes strongly with existing treatments like Venetoclax or Azacytidine, as well as with emerging Menin inhibitors (such as bleximenib) to achieve deep tumor growth inhibition
Lasmotinib is an orally bioavailable inhibitor of checkpoint kinase 2 (chk2), with potential antineoplastic and chemopotentiating activities. Upon oral administration, lasmotinib binds to and inhibits the activity of chk2, which may prevent the repair of DNA damage caused by DNA-damaging agents. This may result in tumor cell apoptosis and potentiate the antitumor efficacies of various chemotherapeutic agents. Chk2, an ATP-dependent serine–threonine kinase, is a key component in the DNA replication-monitoring checkpoint system and is activated by double-stranded breaks (DSBs); activated chk2 is overexpressed by a variety of cancer cell types.
- Chk2 Inhibitor for Recurrent EpitheliAl periToneal, fallopIan or oVarian cancEr (CREATIVE Phase IA Trial)CTID: NCT04678102Phase: Phase 1Status: Unknown statusDate: 2023-06-26
- Evaluation of the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of PHI 101 for the Treatment of AMLCTID: NCT04842370Phase: Phase 1Status: Unknown statusDate: 2021-04-20
PAT
https://patentscope.wipo.int/search/en/detail.jsf?docId=JP405710409&_cid=P21-MQIVJB-43702-2
PAT
https://patentscope.wipo.int/search/en/detail.jsf?docId=US465154324&_cid=P21-MQIVJB-43702-2
SYN
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2024015484&_cid=P21-MQIVJB-43702-2
PAT
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2025210599&_cid=P21-MQIVJB-43702-2
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////////lasmotinib, anax labs, tyrosine kinase inhibitor, antineoplastic, PHI-101, PHI 101, U2UY9TBQ8Z