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FAK is the kinase that tells a cell it is anchored to its surroundings, letting it survive, move and resist drugs. Defactinib, given with the RAF/MEK inhibitor avutometinib, removes that escape route in low-grade serous ovarian cancer; other FAK inhibitors are in trials in meningioma and solid tumours.
PTK2 (chromosome 8q24.3) encodes focal adhesion kinase 1, a non-receptor tyrosine kinase essential for cell migration, adhesion and spreading, actin reorganisation, the assembly and disassembly of focal adhesions, cell-cycle progression, proliferation and apoptosis; it transduces integrin signals and signals from growth-factor receptors, G protein-coupled receptors, EPHA2, netrin and LDL receptors, and is required for embryonic angiogenesis (UniProt Q05397). In OnCo, FAK is blocked by defactinib in the approved avutometinib-defactinib combination for KRAS-mutant low-grade serous ovarian cancer, where it removes an adhesion-driven escape route from MEK inhibition; by GSK2256098 in meningiomas that have lost the NF2 tumour suppressor merlin and depend on FAK (a synthetic-lethal approach); and by IN10018 in phase 3.
In plain words · FAK is the kinase that tells a cell it is anchored to its surroundings, letting it survive, move and resist drugs. Defactinib, given with the RAF/MEK inhibitor avutometinib, removes that escape route in low-grade serous ovarian cancer; other FAK inhibitors are in trials in meningioma and solid tumours.
FAK is the kinase that tells a cell it is anchored to its surroundings, letting it survive, move and resist drugs. Defactinib, given with the RAF/MEK inhibitor avutometinib, removes that escape route in low-grade serous ovarian cancer; other FAK inhibitors are in trials in meningioma and solid tumours.
The corpus records frame FAK as a resistance node rather than a driver: LGSOC cells arrest and regress only when FAK is blocked alongside RAF-MEK, and NF2-deficient meningioma depends on FAK signalling once merlin is lost.
3 products aim at FAK (PTK2): small molecules. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
Broadly expressed or essential: HPA lists PTK2 among essential proteins and finds the RNA at low tissue specificity; the 3 medicines aimed at it (Avutometinib + defactinib, GSK2256098, IN10018) act on the wild-type protein, so normal tissue is exposed and the therapeutic window comes from the tumour's faster division or its dependence on the protein. HPA PTK2: RNA low tissue specificity; high antibody staining in 3 normal tissues; highest cancer staining urothelial cancer (1 of 11 high). Distribution: 4 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Ovarian cancer, Brain and spinal cord tumours (all types), Pancreatic ductal adenocarcinoma, Lung cancer (all types)); Open Targets associates it with 0 specific cancer types at or above 0.5. (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas PTK2 tissue; Open Targets ENSG00000169398 associations
First described 1993. Earliest sequence paper UniProt cites for the protein: Whitney G.S. et al, DNA Cell Biol, 1993, "Human T and B lymphocytes express a structurally conserved focal adhesion kinase, pp125FAK". Source.
The corpus records frame FAK as a resistance node rather than a driver: LGSOC cells arrest and regress only when FAK is blocked alongside RAF-MEK, and NF2-deficient meningioma depends on FAK signalling once merlin is lost.
RNA: low tissue specificity, detected in all normal tissues.
Medium: Adrenal gland, Appendix, Breast, Bronchus, Cerebellum, Colon, Duodenum, Endometrium.
Medium only: breast cancer, carcinoid, cervical cancer, colorectal cancer.
HPA PTK2 tissue · HPA PTK2 pathology · HPA protein class: Essential proteins
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
Avutometinib plus defactinib is the first treatment approved specifically for low-grade serous ovarian cancer, a slow-growing type driven by the RAS pathway.
GSK2256098 is a tablet that blocks an enzyme called FAK, which meningiomas missing the NF2 gene rely on. In the Alliance A071401 trial it slowed progression in recurrent NF2-mutant meningiomas, one of the first positive results for a targeted drug in this tumour.
IN10018 is an experimental small-molecule drug from InxMed (Shanghai) in phase 3 trials for non-small-cell lung cancer, pancreatic ductal adenocarcinoma and ovarian cancer, with its target not yet stated publicly.
Query for this target: (TITLE:"FAK" OR ABSTRACT:"FAK" OR TITLE:"PTK2" OR ABSTRACT:"PTK2" OR TITLE:"FAK1" OR ABSTRACT:"FAK1" OR TITLE:"FADK" OR ABSTRACT:"FADK" OR TITLE:"focal adhesion kinase" OR ABSTRACT:"focal adhesion kinase" OR TITLE:"protein tyrosine kinase 2" OR ABSTRACT:"protein tyrosine kinase 2") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about FAK (PTK2), not a curated reading list.
Shares Resistance routes: how a blocked pathway comes back, KRAS, Small-molecule kinase inhibitors, Pancreatic ductal adenocarcinoma and the tag wave5-target.
Shares MEK1/2, KRAS, Small-molecule kinase inhibitors, Non-small-cell lung cancer and the tag wave5-target.
Shares Small-molecule kinase inhibitors and the tag wave5-target.
Shares Small-molecule kinase inhibitors and the tag wave5-target.
Shares Ovarian cancer and the tag wave5-target.
Shares Small-molecule kinase inhibitors and the tag wave5-target.
Shares Non-small-cell lung cancer and the tag wave5-target.