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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). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
KX2-391 | KX-01|Tirbanibulin | FLT3 Inhibitor 69 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). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
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 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 |
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 | 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 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 | 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 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 |
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 |
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 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 |
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 | Completed | USA | 0 |