NK1 receptor (TACR1)
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.
Overview
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.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
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.
- 1 · What it is
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.
- 2 · What goes wrong in cancer
G protein-coupled receptor for substance P in the nucleus tractus solitarius and area postrema; blocked by pitant antiemetics.
- 3 · How drugs use it
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.
External identifiers
Biology
G protein-coupled receptor for substance P in the nucleus tractus solitarius and area postrema; blocked by pitant antiemetics.
- Supportive care: prevention of delayed chemotherapy-induced nausea and vomiting
Latest papers
topQuery 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.
Similar pages
not linked directly; found by shared links- TreatmentRolapitant
Shares Netupitant and palonosetron, Aprepitant (and fosaprepitant).
- TreatmentPalonosetron
Shares Netupitant and palonosetron, Aprepitant (and fosaprepitant).
- TechnologyAntiemetics for chemotherapy-induced nausea and vomiting
Shares Netupitant and palonosetron, Aprepitant (and fosaprepitant).