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The substance P receptor that drives the delayed nausea felt in the days after chemotherapy. Aprepitant and netupitant block it and are combined with a 5-HT3 blocker and dexamethasone for the most nausea-provoking regimens.
Substance P acting on neurokinin 1 receptors in the brainstem mediates the delayed phase of chemotherapy-induced nausea and vomiting, which 5-HT3 antagonists control poorly. Aprepitant, approved in 2003, was the first NK1 antagonist; fosaprepitant, rolapitant and the netupitant-palonosetron combination followed. Adding an NK1 antagonist to a 5-HT3 antagonist and dexamethasone is the guideline standard for highly emetogenic chemotherapy such as cisplatin and anthracycline-cyclophosphamide, and it interacts with drugs metabolised by CYP3A4, so dexamethasone doses are reduced.
In plain words · The substance P receptor that drives the delayed nausea felt in the days after chemotherapy. Aprepitant and netupitant block it and are combined with a 5-HT3 blocker and dexamethasone for the most nausea-provoking regimens.
The substance P receptor that drives the delayed nausea felt in the days after chemotherapy. Aprepitant and netupitant block it and are combined with a 5-HT3 blocker and dexamethasone for the most nausea-provoking regimens.
G protein-coupled receptor for substance P in the nucleus tractus solitarius and area postrema; blocked by pitant antiemetics.
No product in this corpus aims at NK1 receptor (TACR1) yet. Drugs bind the molecule precisely: to switch it off, flag the cell for the immune system, or deliver a payload.
Tumour-associated overexpression: HPA finds the RNA tissue enhanced in normal adipose tissue, so the tumour and the normal tissue it comes from share the target and the medicine relies on the difference in level. HPA TACR1: RNA tissue enhanced (adipose tissue 6 nTPM); blood lineage lineage enriched (granulocytes 2 nTPM); no normal tissue stained high; highest cancer staining skin cancer (1 of 12 high). Distribution: no corpus cancer carries a prevalence row, threshold or catalogue link for it; 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 TACR1 tissue; Human Protein Atlas TACR1 pathology; Open Targets ENSG00000115353 associations
First described 1991. Earliest sequence paper UniProt cites for the protein: Takeda et al, Biochem. Biophys. Res. Commun, 1991, "Molecular cloning, structural characterization and functional expression of the human substance P receptor". Source.
G protein-coupled receptor for substance P in the nucleus tractus solitarius and area postrema; blocked by pitant antiemetics.
RNA: tissue enhanced (adipose tissue 6 nTPM), detected in many normal tissues. Blood: lineage enriched (granulocytes 2 nTPM).
No normal tissue stained high; medium in Bronchus, Cervix, Esophagus, Prostate, Skin, Vagina.
HPA TACR1 tissue · HPA TACR1 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 |
|---|---|---|---|---|
| Metastatic cancer | host% | Host target: substance P receptor in the vomiting pathway. Not a tumour alteration, so no prevalence applies; the drug acts on normal tissue or on symptoms. |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Query for this target: (TITLE:"NK1 receptor" OR ABSTRACT:"NK1 receptor" OR TITLE:"TACR1" OR ABSTRACT:"TACR1") 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 NK1 receptor (TACR1), not a curated reading list.
Shares Netupitant and palonosetron, Dexamethasone.
Shares 5-HT3 receptor (HTR3A), Netupitant and palonosetron, Aprepitant (and fosaprepitant).
Shares Netupitant and palonosetron, Dexamethasone.
Shares Rolapitant, Dexamethasone.
Shares 5-HT3 receptor (HTR3A), Aprepitant (and fosaprepitant).
Shares Rolapitant, Netupitant and palonosetron, Aprepitant (and fosaprepitant), Dexamethasone.