THERAPY DOSSIER · th-4c80917d0a14

LY303870 (selective neurokinin-1 receptor antagonist)

Drug · ChEMBL get_mechanism returned ZERO curated records for CHEMBL42407, so no mechanism is asserted here. ChEMBL does assign the USAN stem -tant (-pitant), defined as tachykinin (neurokinin) receptor antagonists: NK1 receptor antagonists, which is consistent with the source description but is a naming-convention annotation, not a curated mechanism record.

Not approved Suggest a correction

Evidence & regulatory context

Mechanism: ChEMBL get_mechanism returned ZERO curated records for CHEMBL42407, so no mechanism is asserted here. ChEMBL does assign the USAN stem -tant (-pitant), defined as tachykinin (neurokinin) receptor antagonists: NK1 receptor antagonists, which is consistent with the source description but is a naming-convention annotation, not a curated mechanism record.
Target: Not recorded
Injury models: Fracture
Reported indication: Not recorded
First approval: Not recorded
Development stage: Preclinical/no trial
ChEMBL record: CHEMBL42407 ↗
ChEMBL max phase: 2 / 4 (development scale, not regulatory approval)
Synonyms: Lanepitant; LY303870
Note: Not recorded

Clinical trials 0

0 linked trials carry an injury-indication flag. These flags support record-level exploration and sit alongside the stringent aggregate counts described in Methods.

No linked human trial in this dataset.

Preclinical evidence 1

1 studies reported at therapy level; 1 evidence entries itemised.

PMID 22343473 ↗2012Reported benefit

Substance P signaling controls mast cell activation, degranulation, and nociceptive sensitization in a rat fracture model of complex regional pain syndrome.

RatFractureTibiaSprague Dawley (Simonsen Laboratories)Malen = Groups of 6 to 10 rats; sciatic nerve stimulation experimen…Intraperitoneal20 mg/kg/day intraperitoneally; 30 to 40 mg/kg intraperiton…Given for 8 days before euthanasia at the end of the 4-week cast period; in the…

Model: Distal tibia fracture created with modified pliers followed by 4 weeks of hindlimb cast immobilisation (rat model of complex regional pain syndrome type I)

Fracture produced a roughly fourfold increase in dermal mast cell number and a 250 per cent increase in degranulation; LY303870 completely reversed the fracture-induced increase in mast cell number and neurokinin-1 receptor expression and blocked mast cell degranulation and nociceptive sensitisatio…

Extraction: extract · Subtype source: rule · Supplied extraction confidence: 0.9. Machine-extracted fields require source verification.

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LY303870 (selective neurokinin-1 receptor antagonist)