Lufotrelvir

Summary

Lufotrelvir (CHEMBL4802214) is a phase-3 clinical-stage small-molecule prodrug; indicated across 2 conditions including severe acute respiratory syndrome and viral infectious disease.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 2 conditions
• Clinical trials: 5
• Chemistry: 552.5 Da · C24H33N4O9P

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4802214
Name	Lufotrelvir
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	154699467
ChEBI	CHEBI:173073
Molecular formula	C24H33N4O9P
Molecular weight	552.5
InChIKey	FQKALOFOWPDTED-WBAXXEDZSA-N

SMILES: CC(C)C[C@@H](C(=O)N[C@@H](C[C@@H]1CCNC1=O)C(=O)COP(=O)(O)O)NC(=O)C2=CC3=C(N2)C=CC=C3OC

IUPAC name: [(3S)-3-[[(2S)-2-[(4-methoxy-1H-indole-2-carbonyl)amino]-4-methylpentanoyl]amino]-2-oxo-4-[(3S)-2-oxopyrrolidin-3-yl]butyl] dihydrogen phosphate

ChEBI definition: An indolecarboxamide resulting from the formal condensation of the carboxy group of 4-methoxy-1H-indole-2-carboxylic acid with the primary amino group of N-[(2S)-3-oxo-1-[(3S)-2-oxopyrrolidin-3-yl]-4-(phosphonooxy)butan-2-yl]-L-leucinamide. It is the phosphate prodrug of PF-00835231, an anticoronaviral agent.

Pharmacological roles (ChEBI): prodrug, EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor, anticoronaviral agent.

Also known as: Lufotrelvir, Pf-07304814, PF-07304814, PF07304814, LUFOTRELVIR

Patent coverage: 96 distinct patent families (220 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 204 (93%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Replicase polyprotein 1ab.

Bioactivity

ChEMBL activities: 1 potent at pChembl ≥ 5 of 1 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P0DTD1	6.76	Ki	174	nM	CHEMBL_ACT_25061595

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

2 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
severe acute respiratory syndrome	3	MONDO:0005091	MONDO:0100096
viral infectious disease	1	MONDO:0005108	EFO:0000763

Clinical trials

Total trials: 5.

Phase distribution

Phase	Trials
PHASE1	3
PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04501978	PHASE3	COMPLETED	ACTIV-3: Therapeutics for Inpatients With COVID-19
NCT05780541	PHASE3	TERMINATED	PF-07304814 for Inpatients With COVID-19 (An ACTIV-3/TICO Treatment Trial)
NCT04535167	PHASE1	COMPLETED	First-In-Human Study To Evaluate Safety, Tolerability, And Pharmacokinetics Following Single Ascending And Multiple Ascending Doses of PF-07304814 In Hospitalized Participants With COVID-19.
NCT04627532	PHASE1	COMPLETED	Single Ascending Dose Study of Intravenous Infusion of PF 07304814 in Healthy Adult Participants
NCT05050682	PHASE1	COMPLETED	Study to Investigate the Mass Balance, Metabolism, and Excretion of [14C]-PF-07304814 in Healthy Participants

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).