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Folate receptor alpha is a vitamin receptor that ovarian cancer cells carry in large numbers, used as the docking site for the ADC mirvetuximab.
FRα is overexpressed in high-grade serous ovarian cancer, endometrial cancer, and lung adenocarcinoma. Mirvetuximab soravtansine (Elahere) is approved in FRα-high platinum-resistant ovarian cancer (MIRASOL). Next-generation FRα ADCs with topoisomerase-I payloads (ZW191, luveltamab tazevibulin, rinatabart sesutecan) target lower-expressing tumours.
In plain words · Folate receptor alpha is a vitamin receptor that ovarian cancer cells carry in large numbers, used as the docking site for the ADC mirvetuximab.
Folate receptor alpha is a vitamin receptor that ovarian cancer cells carry in large numbers, used as the docking site for the ADC mirvetuximab.
GPI-anchored folate transporter; limited to apical surfaces in normal kidney, lung, and choroid plexus.
7 products aim at Folate receptor alpha: antibody-drug conjugates, small molecules and imaging agents. Because it sits on the outside of the cell, it can be reached from the bloodstream: antibodies flag the cell, ADCs deliver a toxin, radioligands deliver radiation, and CAR-T or bispecifics bring a T cell.
Tumour-associated overexpression or amplification: 1 of 1 label readouts filed under it score protein level or gene copies (Folate receptor alpha expression (FRα-positive, PS2+ >= 75%)), so the medicines rely on the tumour carrying more of it than normal tissue. HPA FOLR1: RNA tissue enriched (choroid plexus 2,861 nTPM); no normal tissue stained high. Distribution: 3 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Ovarian cancer, Endometrial cancer, Lung cancer (all types)); Open Targets associates it with 1 specific cancer type at or above 0.5 (ovarian cancer). (Rule 3 of scripts/fetch-target-specificity.ts.)
Sources: Folate receptor alpha expression (FRα-positive, PS2+ >= 75%) label threshold; Human Protein Atlas FOLR1 tissue; Human Protein Atlas FOLR1 pathology; Open Targets ENSG00000110195 associations
First described 1987. Earliest sequence paper UniProt cites for the protein: Luhrs C.A. et al, Proc. Natl. Acad. Sci. U.S.A, 1987, "Purified membrane and soluble folate binding proteins from cultured KB cells have similar amino acid compositions and molecular weights but differ in fatty acid acylation". Source.
What a pathology or genomic report can say about this target, each with the thresholds approvals use.
GPI-anchored folate transporter; limited to apical surfaces in normal kidney, lung, and choroid plexus.
RNA: tissue enriched (choroid plexus 2,861 nTPM), detected in many normal tissues.
No normal tissue stained high.
RNA cancer enhanced: Ovary Serous Cystadenocarcinoma 633 pTPM.
No cancer sample stained medium or high.
HPA FOLR1 tissue · HPA FOLR1 pathology · HPA protein class: FDA approved drug targets
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.
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Non-small-cell lung cancer | 70-80% | Adenocarcinoma, any expression | Wikipedia | |
| Endometrial cancer | 60-80% | IHC, any expression | Wikipedia | |
| Ovarian cancer | 35-40% | FRα-high (PS2+ in >=75% of cells) | MIRASOL eligibility; ~80% any expression | Wikipedia |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Chiauranib is an experimental small-molecule drug from Chipscreen Biosciences in phase 3 trials for ovarian cancer, aimed at VEGF / VEGFR and KIT.
Farletuzumab-exatecan is an experimental antibody-drug conjugate from CSPC Megalith Biopharmaceutical in phase 2 trials, aimed at Folate receptor alpha.
A folate-receptor ADC designed to work across low and high receptor levels, in a pivotal ovarian cancer trial.
Mirvetuximab soravtansine (Elahere) is the first ADC for ovarian cancer, for tumours with high folate receptor alpha.
An injected dye that makes ovarian and lung cancer deposits glow during surgery so surgeons can find lesions they would otherwise miss.
Rinatabart sesutecan is a next-generation folate-receptor ADC with a topoisomerase payload that responds in both ovarian and endometrial cancer regardless of receptor level.
Sofetabart Mipitecan is an experimental antibody-drug conjugate from Eli Lilly and in phase 3 trials for ovarian cancer, aimed at Folate receptor alpha.
Query for this target: (TITLE:"Folate receptor alpha" OR ABSTRACT:"Folate receptor alpha" OR TITLE:"FOLR1" OR ABSTRACT:"FOLR1") 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 Folate receptor alpha, not a curated reading list.
Shares Sutro Biopharma, Antibody-drug conjugate (ADC) and the tag adc-target.
Shares Mitosis & the spindle assembly checkpoint, Antibody-drug conjugate (ADC), Triple-negative breast cancer (TNBC) and the tag adc-target.
Shares Antibody-drug conjugate (ADC), Ovarian cancer and the tag adc-target.
Shares Re-map the tumour's surface proteins before choosing the next antibody drug, Antibody-drug conjugate (ADC) and the tag adc-target.
Shares Antibody-drug conjugate (ADC), Triple-negative breast cancer (TNBC) and the tag adc-target.
Shares Mitosis & the spindle assembly checkpoint, Antibody-drug conjugate (ADC) and the tag adc-target.
Shares Antibody-drug conjugate (ADC) and the tag adc-target.
Shares Antibody-drug conjugate (ADC) and the tag adc-target.