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Therapy Name KX2-391
Synonyms
Therapy Description

Tirbanibulin (KX2-391) is a peptidomimetic inhibitor of Src and pretubulin, with additional activity against FLT3, potentially resulting in decreased tumor growth and metastasis (PMID: 22784709, PMID: 31628188, PMID: 34217323).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
KX2-391 KX-01|Tirbanibulin FLT3 Inhibitor 66 SRC Inhibitor 31 Tirbanibulin (KX2-391) is a peptidomimetic inhibitor of Src and pretubulin, with additional activity against FLT3, potentially resulting in decreased tumor growth and metastasis (PMID: 22784709, PMID: 31628188, PMID: 34217323).

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  • Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
PTEN G129R ovarian mucinous neoplasm decreased response KX2-391 Preclinical Actionable In a preclincal study, mucinous ovarian carcinoma cell lines over-expressing PTEN G129R were less sensitive to KX2-391 induced growth inhibition in culture and tumor suppression in xenograft models (PMID: 24100628). 24100628
FLT3 exon 14 ins FLT3 D835F hematologic cancer sensitive KX2-391 Preclinical - Cell culture Actionable In a preclinical study, KX2-391 treatment inhibited cell viability and decreased downstream signaling in cells expressing a FLT3-ITD mutation with FLT3 D835F in culture (PMID: 34217323). 34217323
FLT3 exon 14 ins acute myeloid leukemia sensitive KX2-391 Preclinical - Patient cell culture Actionable In a preclinical study, KX2-391 treatment inhibited cell viability and decreased downstream signaling in acute myeloid leukemia cell lines and patient-derived cells harboring a FLT3-ITD mutation in culture (PMID: 34217323). 34217323
PTEN loss ovarian mucinous neoplasm decreased response KX2-391 Preclinical Actionable In a preclincal study, mucinous ovarian carcinoma cell lines harboring PTEN loss were less sensitive to KX2-391 induced growth inhibition in culture and tumor suppression in xenograft models (PMID: 24100628). 24100628
FLT3 exon 14 ins FLT3 D835Y hematologic cancer sensitive KX2-391 Preclinical - Cell culture Actionable In a preclinical study, KX2-391 treatment inhibited cell viability, decreased downstream signaling, and induced apoptosis in cells expressing a FLT3-ITD mutation with FLT3 D835Y in culture (PMID: 34217323). 34217323
FLT3 exon 14 ins FLT3 D835Y acute myeloid leukemia predicted - sensitive KX2-391 Preclinical - Patient cell culture Actionable In a preclinical study, KX2-391 treatment inhibited cell viability and decreased Flt3 phosphorylation in patient-derived acute myeloid leukemia cell lines harboring a FLT3-ITD mutation with FLT3 D835Y in culture (PMID: 34217323). 34217323
PTEN wild-type ovarian mucinous neoplasm sensitive KX2-391 Preclinical Actionable In a preclinical study, KX2-391 inhibited survival of PTEN wild-type mucinous ovarian carcinoma cell lines in culture, and reduced tumor growth in xenograft models (PMID: 24100628). 24100628
FLT3 exon 14 ins FLT3 D835V hematologic cancer sensitive KX2-391 Preclinical - Cell culture Actionable In a preclinical study, KX2-391 treatment inhibited cell viability and decreased downstream signaling in cells expressing a FLT3-ITD mutation with FLT3 D835V in culture (PMID: 34217323). 34217323
FLT3 exon 14 ins hematologic cancer sensitive KX2-391 Preclinical - Cell culture Actionable In a preclinical study, KX2-391 treatment inhibited cell viability, decreased downstream signaling, and induced apoptosis in cells expressing a FLT3-ITD mutation in culture (PMID: 34217323). 34217323
FLT3 exon 14 ins FLT3 F691L hematologic cancer sensitive KX2-391 Preclinical Actionable In a preclinical study, KX2-391 treatment inhibited viability, decreased downstream signaling, and induced apoptosis in cells expressing a FLT3-ITD mutation with FLT3 F691L in culture, and inhibited tumor growth and prolonged survival in mouse models (PMID: 34217323). 34217323

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT06112522 Phase II KX2-391 Tirbanubulin (Klisiry) in the Treatment of Basal Cell Carcinoma Recruiting FRA 0
NCT05713760 Phase II KX2-391 Proof of Concept Study to Access Superficial Basal Cell Carcinoma in Adults Recruiting USA 0


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