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Atlas / Drug / Milvexian

Milvexian

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Also known as BMS 986177Bms-986177Jnj-70033093

Summary

Milvexian (CHEMBL4112929) is a phase-3 clinical-stage small molecule targeting CTRC, F11, and KLKB1; indicated across 3 conditions including atrial fibrillation and acute coronary syndrome.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 3 (CTRC, F11, KLKB1)
  • Indications: 3 conditions
  • Clinical trials: 26
  • Chemistry: 626.4 Da · C28H23Cl2F2N9O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL4112929
NameMilvexian
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID118277544
Molecular formulaC28H23Cl2F2N9O2
Molecular weight626.4
InChIKeyFSWFYCYPTDLKON-CMJOXMDJSA-N

SMILES: C[C@@H]1CCC[C@@H](C2=NC=CC(=C2)C3=C(C=NN3C(F)F)NC1=O)N4C=NC(=CC4=O)C5=C(C=CC(=C5)Cl)N6C=C(N=N6)Cl

IUPAC name: (9R,13S)-13-[4-[5-chloro-2-(4-chlorotriazol-1-yl)phenyl]-6-oxopyrimidin-1-yl]-3-(difluoromethyl)-9-methyl-3,4,7,15-tetrazatricyclo[12.3.1.02,6]octadeca-1(18),2(6),4,14,16-pentaen-8-one

Also known as: BMS 986177, Bms-986177, BMS-986177, Jnj-70033093, JNJ-70033093, Milvexian, MILVEXIAN

Patent coverage: 61 distinct patent families (134 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 88 (66%) 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

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
CTRCchymotrypsin CInhibition7.460.1%Q99895
F11coagulation factor XIInhibition9.960.2%P03951
KLKB1kallikrein B1Inhibition7.360%P03952

Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: Plasminogen, Tissue-type plasminogen activator, Plasma kallikrein, Prothrombin, Trypsin, Coagulation factor XI, Urokinase-type plasminogen activator, Coagulation factor VII, Chymotrypsin.

Bioactivity

ChEMBL activities: 19 potent at pChembl ≥ 5 of 19 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
F1110Ki0.1nMCHEMBL_ACT_17791791
F1110Ki0.1nMCHEMBL_ACT_27702500
F1110Ki0.1nMCHEMBL_ACT_28484315
F119.96Ki0.11nMCHEMBL_ACT_24387455
F119.96Ki0.11nMCHEMBL_ACT_25530195
F119.96Ki0.11nMCHEMBL_ACT_29077888
F119.96Ki0.11nMCHEMBL_ACT_29112189
KLKB17.55Ki28nMCHEMBL_ACT_17791802
KLKB17.55Ki28nMCHEMBL_ACT_26643133
KLKB17.55Ki28nMCHEMBL_ACT_28484348
CTRB17.46Ki35nMCHEMBL_ACT_24387431
KLKB17.36Ki44nMCHEMBL_ACT_24387518
KLKB17.36Ki44nMCHEMBL_ACT_29112194
PRSS16.14Ki720nMCHEMBL_ACT_24387521
F75.92Ki1200nMCHEMBL_ACT_24387514
F25.92Ki1200nMCHEMBL_ACT_24387520
PLAT5.64Ki2300nMCHEMBL_ACT_24387524
PLG5.58Ki2650nMCHEMBL_ACT_24387523
PLAU5.41Ki3900nMCHEMBL_ACT_24387525

Target pathways

Aggregated over 3 target gene(s): CTRC, F11, KLKB1.

Top Reactome pathways

18 total, by targets touching each:

PathwayTargetsGenes
R-HSA-1408372F11, KLKB1
FXIIa, PKa-dependent activation of coagulation pathway2F11, KLKB1
Hemostasis1KLKB1
R-HSA-1408771KLKB1
Degradation of the extracellular matrix1KLKB1
Extracellular matrix organization1KLKB1
Activation of Matrix Metalloproteinases1KLKB1
Disease1KLKB1
R-HSA-96514961KLKB1
Defective factor XII causes hereditary angioedema1KLKB1
Defective SERPING1 causes hereditary angioedema1KLKB1
Diseases of hemostasis1KLKB1
Defective F9 activation1F11
Regulation of clotting cascade1F11
Amplification and propagation of coagulation cascade1F11
Regulation of FXIIa and plasma kallikrein activity1KLKB1
Developmental Lineage of Pancreatic Acinar Cells1CTRC
FXIIa activates plasma kallikrein-kinin system1KLKB1

Dominant GO biological processes

GO termTargets
proteolysis3
blood coagulation2
plasminogen activation2
positive regulation of fibrinolysis2
hemostasis2
intracellular calcium ion homeostasis1
regulation of blood coagulation1
Factor XII activation1
zymogen activation1
fibrinolysis1
inflammatory response1

Indications & clinical

Indications

3 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).

IndicationTrial phaseMONDOEFO
atrial fibrillation3MONDO:0004981EFO:0000275
acute coronary syndrome3MONDO:0005542EFO:0005672
thrombotic disease1MONDO:0000831MONDO:0000831

Clinical trials

Total trials: 26.

Phase distribution

PhaseTrials
PHASE120
PHASE33
PHASE22
PHASE1/PHASE21

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05702034PHASE3ACTIVE_NOT_RECRUITINGA Study of Milvexian in Participants After an Acute Ischemic Stroke or High-Risk Transient Ischemic Attack- LIBREXIA-STROKE
NCT05757869PHASE3ACTIVE_NOT_RECRUITINGA Study of Milvexian Versus Apixaban in Participants With Atrial Fibrillation
NCT05754957PHASE3COMPLETEDA Study of Milvexian in Participants After a Recent Acute Coronary Syndrome
NCT03000673PHASE1/PHASE2COMPLETEDA Study to Evaluate Safety of Single Doses of BMS-986177 in Patients With End Stage Renal Disease (ESRD) Treated With Hemodialysis
NCT03766581PHASE2COMPLETEDA Study on BMS-986177 for the Prevention of a Stroke in Patients Receiving Aspirin and Clopidogrel
NCT03891524PHASE2COMPLETEDA Study of JNJ-70033093 (BMS-986177) Versus Subcutaneous Enoxaparin in Participants Undergoing Elective Total Knee Replacement Surgery
NCT02608970PHASE1COMPLETEDSafety and Tolerability Study of BMS-986177 in Healthy Subjects
NCT02807909PHASE1COMPLETEDA Study to Evaluate the Effect of Co-administration of Itraconazole or Diltiazem on the Pharmacokinetics of BMS-986177 in Healthy Subjects
NCT02902679PHASE1COMPLETEDA Study to Evaluate the Safety and Pharmacokinetics of BMS-986177 in Participants With End-stage Renal Dysfunction on Chronic Stable Hemodialysis Treatment
NCT02959060PHASE1COMPLETEDA Study to Evaluate the Effect of Rifampin on the Single-dose Pharmacokinetics of BMS-986177 in Healthy Subjects
NCT02982707PHASE1COMPLETEDSingle-dose Pharmacokinetics of BMS-986177 in Participants With Hepatic Impairment Compared to Healthy Participants
NCT03196206PHASE1COMPLETEDEvaluate Pharmacokinetics and Safety of BMS-986177 in Participants With Normal Renal Function and With Moderate or Severe Renal Impairment
NCT03224260PHASE1COMPLETEDTo Evaluate the Safety and Pharmacokinetics of BMS-986177 in Healthy Japanese Participants
NCT03341390PHASE1COMPLETEDAn Investigational Study to Assess the Effect of BMS-986177 on Aspirin in Healthy Participants
NCT03362437PHASE1COMPLETEDEvaluate the Pharmacokinetics of BMS-986177 From Two Formulations in Healthy Participants
NCT03698513PHASE1COMPLETEDA Study to Assess Administration of an Oral Anti-thrombotic With Antiplatelet Therapy in Healthy Subjects
NCT03939702PHASE1COMPLETEDPharmacokinetic and Metabolism of [14^C] BMS-986177 in Healthy Male Participants
NCT04206488PHASE1COMPLETEDA Study of JNJ-70033093 and Digoxin in Healthy Participants
NCT04223349PHASE1COMPLETEDA Study of JNJ-70033093 (BMS-986177) in Healthy Adult Participants
NCT04388501PHASE1COMPLETEDA Study Evaluating Drug Drug Interaction Between Milvexian and Atorvastatin in Healthy Participants
NCT04448964PHASE1COMPLETEDA Study of JNJ-70033093 in Healthy Participants
NCT04543383PHASE1COMPLETEDA Study to Assess the Reversal of the Anticoagulant Effects of Milvexian by 4-Factor Prothrombin Complex Concentrate (4F-PCC) (Part 1) and Recombinant Human Factor VIIa (rFVIIa) (Part 2) in Healthy Participants
NCT04569695PHASE1COMPLETEDA Study of JNJ-70033093 (BMS-986177) in Healthy Chinese Adult Participants
NCT04844424PHASE1COMPLETEDA Study of JNJ-70033093 (Milvexian) in Healthy Adult Participants
NCT04965389PHASE1COMPLETEDA Study of Milvexian Using an IV Microtracer With Additional Formulation and Food Effect Comparison in Healthy Participants
NCT05706753PHASE1COMPLETEDA Study of Milvexian in Healthy Adult Females

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

49 molecules share ≥1 primary target. Top 49 by shared-target count:

MoleculeSourceStatusShared targets
AmiloridePubChemApprovedF11, KLKB1
BEROTRALSTATChEMBL + PubChemPhase 4 (approved)KLKB1
MELAGATRANChEMBLPhase 4 (approved)F11
QUERCETINChEMBL + PubChemPhase 3 (approved)CTRC
AVORALSTATChEMBLPhase 3KLKB1
DAREXABANChEMBLPhase 3KLKB1
GABEXATEChEMBLPhase 3KLKB1
SEBETRALSTATChEMBLPhase 3KLKB1
FENIRALSTATChEMBLPhase 2KLKB1
FRUNEXIANChEMBLPhase 2F11
GW813893ChEMBLPhase 2KLKB1
IODOPHTHALEINChEMBLPhase 2CTRC
LETAXABANChEMBLPhase 2KLKB1
Azelaic AcidPubChemApprovedCTRC
CarbamazepinePubChemApprovedCTRC
CarfilzomibPubChemApprovedCTRC
CarisoprodolPubChemApprovedCTRC
ChlorambucilPubChemApprovedCTRC
ChlorthalidonePubChemApprovedCTRC
DapsonePubChemApprovedCTRC
DeferoxaminePubChemApprovedCTRC
DiflunisalPubChemApprovedCTRC
DiphenhydraminePubChemApprovedCTRC
EtodolacPubChemApprovedCTRC
FlutamidePubChemApprovedCTRC
FurosemidePubChemApprovedCTRC
GemfibrozilPubChemApprovedCTRC
GuaifenesinPubChemApprovedCTRC
GuanabenzPubChemApprovedCTRC
IndomethacinPubChemApprovedCTRC
LamotriginePubChemApprovedCTRC
LansoprazolePubChemApprovedCTRC
LeflunomidePubChemApprovedCTRC
LidocainePubChemApprovedCTRC
MebendazolePubChemApprovedCTRC
mesalaminePubChemApprovedCTRC
NitrofurantoinPubChemApprovedCTRC
OndansetronPubChemApprovedCTRC
PrazosinPubChemApprovedCTRC
PrimidonePubChemApprovedCTRC
ProtriptylinePubChemApprovedCTRC
RiboflavinPubChemApprovedCTRC
RiluzolePubChemApprovedCTRC
SulfadiazinePubChemApprovedCTRC
ThalidomidePubChemApprovedCTRC
torsemidePubChemApprovedCTRC
TriamterenePubChemApprovedCTRC
TrimethoprimPubChemApprovedCTRC
TripelennaminePubChemApprovedCTRC

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot