Biomarker & Intervention Discovery

Breast Cancer

This page lists 13 druggable gene targets, 44 approved or trial-tested drug candidates and 15 recent clinical trials for Breast Cancer, with each agent ranked by the strength of its evidence (clinical, mechanistic or correlative). Candidates include existing drugs that could be repurposed. Sources are linked so you can check every claim.

US DALYs1.37MWHO GHE 2021 · all ages
Global DALYs22.85MWHO GHE 2021 · worldwide
US mortality48.9K deaths/yrWHO GHE 2021
Global mortality701.9K deaths/yrWHO GHE 2021 · worldwide
NIH funding$757MFY2025 · RCDC estimate
Funding levelModerate
Spontaneous remissionSpontaneous regression documented but rare (<0.5%); 5-year survival stage I: ~99%; stage IV: ~28% overall, improving…
Best-intervention remissionHER2+ metastatic: pertuzumab + trastuzumab + docetaxel (CLEOPATRA: 57.1-month median OS vs 40.8 months); HR+/HER2-…
Gap sizeVaries greatly by subtype; HER2+ and HR+ have dramatically improved outcomes; TNBC lags; metastatic remains incurable…
Primary barrierbiological (metastatic) + access (treatment disparities by race/SES)
Full remission profile →

Remission & chronicity

Spontaneous remission
Spontaneous regression documented but rare (<0.5%); 5-year survival stage I: ~99%; stage IV: ~28% overall, improving with modern therapy
Best-intervention remission
HER2+ metastatic: pertuzumab + trastuzumab + docetaxel (CLEOPATRA: 57.1-month median OS vs 40.8 months); HR+/HER2- with CDK4/6 inhibitors: 63-month PFS in first-line (MONALEESA-2); TNBC with pembrolizumab + chemotherapy: 23-month OS vs 16.1 months; pCR with neoadjuvant: 80-90% in HER2+ with dual HER2 blockade
Gap size
Varies greatly by subtype; HER2+ and HR+ have dramatically improved outcomes; TNBC lags; metastatic remains incurable in most patients
Primary barrier
biological (metastatic) + access (treatment disparities by race/SES)
Racial disparities in breast cancer mortality persist (Black women 40% higher mortality despite similar incidence); access to genetic testing (BRCA1/2) and CDK4/6 inhibitors varies significantly; germline testing vastly underutilised

Biomarker Targets & Therapeutic Agents

Gene targets queried against DGIdb, Open Targets, ChEMBL, PubMed, and Europe PMC. Agents ranked: Clinical > Mechanistic > Correlative.

AKT1 248AR 994BRCA1 283BRCA2 19CDK4 255CDK6 226ERBB2 336ESR1 386PARP1 207PGR 158PIK3CA 444TACSTD2 4TOP2A 289
Therapeutic Agent Effect Direction Evidence Tier Potency Source
FASUDIL ? unclear Mechanistic
TOPOTECAN HYDROCHLORIDE ? unclear Mechanistic
5-METHOXYCANTHINONE ? unclear Mechanistic
IPATASERTIB ↓ inhibits Mechanistic
MS15 ↓ inhibits Mechanistic
NELFINAVIR ↓ inhibits Mechanistic
XL418 ? unclear Mechanistic
ENZASTAURIN ? unclear Mechanistic
TRICIRIBINE ↓ inhibits Mechanistic
PERIFOSINE ↓ inhibits Mechanistic
M-2698 ↓ inhibits Mechanistic
UPROSERTIB ↓ inhibits Mechanistic
CANTHIN-6-ONE ? unclear Mechanistic
CAPIVASERTIB ↓ inhibits Mechanistic
CI-1040 ? unclear Mechanistic
CHEMBL:CHEMBL480356 ? unclear Mechanistic
ANDROGRAPHOLIDE ? unclear Mechanistic
SR-13668 ↓ inhibits Mechanistic
LAUROGUADINE ? unclear Mechanistic
DABRAFENIB ? unclear Mechanistic
GEFITINIB ? unclear Mechanistic
EVEROLIMUS ↓ inhibits Mechanistic
GIGANTOL ? unclear Mechanistic
GSK690693 ↓ inhibits Mechanistic
VAD-044 ~ modulates Mechanistic
HU7691 ↓ inhibits Mechanistic
LY-2780301 ↓ inhibits Mechanistic
GAMBOGIC AMIDE ? unclear Mechanistic
MIRANSERTIB ? unclear Mechanistic
GEDATOLISIB ? unclear Mechanistic
EUPALININ A ? unclear Mechanistic
NINTEDANIB ESYLATE ? unclear Mechanistic
GSK269962A ? unclear Mechanistic
ERLOTINIB ? unclear Mechanistic
CEP-11981 ? unclear Mechanistic
OMIPALISIB ↓ inhibits Mechanistic
A-674563 ↓ inhibits Mechanistic
ARCHEXIN ? unclear Mechanistic
CANERTINIB DIHYDROCHLORIDE ? unclear Mechanistic
BARDOXOLONE METHYL ? unclear Mechanistic

Showing top 40 of 248 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
AMI-1 ? unclear Mechanistic
DIBEKACIN ? unclear Mechanistic
CARBONYL CYANIDE M-CHLOROPHENYLHYDRAZONE ? unclear Mechanistic
TRIPARANOL ? unclear Mechanistic
DODINE ? unclear Mechanistic
TANNIC ACID ? unclear Mechanistic
DEFLAZACORT ? unclear Mechanistic
CHEMBL:CHEMBL1235854 ? unclear Mechanistic
ERGONOVINE ? unclear Mechanistic
AMPEROZIDE HYDROCHLORIDE ? unclear Mechanistic
ATROPINE METHYLBROMIDE ? unclear Mechanistic
ESTRADIOL VALERATE ? unclear Mechanistic
BERBERINE CHLORIDE ? unclear Mechanistic
NITRALIN ? unclear Mechanistic
DEVAZEPIDE ? unclear Mechanistic
MOCLOBEMIDE ? unclear Mechanistic
GLPG0492 ~ modulates Mechanistic
DEUTENZALUTAMIDE ↓ inhibits Mechanistic
PRUXELUTAMIDE ↓ inhibits Mechanistic
HEPTANE ? unclear Mechanistic
THONZONIUM BROMIDE ? unclear Mechanistic
FENHEXAMID ? unclear Mechanistic
LEMILDIPINE ? unclear Mechanistic
(R)-BICALUTAMIDE ? unclear Mechanistic
MORICIZINE HYDROCHLORIDE ? unclear Mechanistic
METIPRANOLOL ? unclear Mechanistic
FLUROCHLORIDONE ? unclear Mechanistic
PYRIDOSTIGMINE BROMIDE ? unclear Mechanistic
FLUTAMIDE ↓ inhibits Mechanistic 154.0 nM (IC50)
CHEMBL:CHEMBL224318 ? unclear Mechanistic
CHEMBL:CHEMBL423081 ? unclear Mechanistic
PREDNISOLONE ? unclear Mechanistic 2760.0 nM (Ki)
ORBIFLOXACIN ? unclear Mechanistic
PROGESTERONE ? unclear Mechanistic 8.5 nM (Ki)
FLUDIOXONIL ? unclear Mechanistic
CHEMBL:CHEMBL1784521 ? unclear Mechanistic
FLUMETHASONE ? unclear Mechanistic
SERTRALINE HYDROCHLORIDE ? unclear Mechanistic
MELOXICAM ? unclear Mechanistic
CHEMBL:CHEMBL44011 ? unclear Mechanistic

Showing top 40 of 994 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
7-HYDROXY ISOFLAVONE ? unclear Mechanistic
OLAPARIB ? unclear Mechanistic
PLATINUM COMPOUND ? unclear Mechanistic
DAIDZIN ? unclear Mechanistic
CHEMBL:CHEMBL581929 ? unclear Mechanistic
PIDNARULEX ? unclear Mechanistic
CHEMBL:CHEMBL1481721 ? unclear Mechanistic
CHEMBL:CHEMBL484663 ? unclear Mechanistic
CHEMBL:CHEMBL1214407 ? unclear Mechanistic
2-PHENYLQUINOLINE ? unclear Mechanistic
HARMALOL ? unclear Mechanistic
CHEMBL:CHEMBL1574420 ? unclear Mechanistic
DOXORUBICIN HYDROCHLORIDE ? unclear Mechanistic
MITOMYCIN ? unclear Mechanistic
PACLITAXEL PROTEIN-BOUND ? unclear Mechanistic
RESVERATROL ? unclear Mechanistic
CHEMBL:CHEMBL12658 ? unclear Mechanistic
ONONIN ? unclear Mechanistic
CEDIRANIB ? unclear Mechanistic
PIPERINE ? unclear Mechanistic
CHEMBL:CHEMBL446567 ? unclear Mechanistic
CHEMBL:CHEMBL546649 ? unclear Mechanistic
DEPHOSTATIN ? unclear Mechanistic
SEMUSTINE ? unclear Mechanistic
CISPLATIN ? unclear Mechanistic
CHEMBL:CHEMBL1404865 ? unclear Mechanistic
QUARFLOXIN ? unclear Mechanistic
PARP/TANKYRASE INHIBITOR 2X-121 ? unclear Mechanistic
WISTIN ? unclear Mechanistic
CHRYSIN DIMETHYL ETHER ? unclear Mechanistic
GEMCITABINE ? unclear Mechanistic
CHEMBL:CHEMBL600315 ? unclear Mechanistic
AURINTRICARBOXYLIC ACID ? unclear Mechanistic
MITOXANTRONE HYDROCHLORIDE ? unclear Mechanistic
SACITUZUMAB GOVITECAN ? unclear Mechanistic
CHEMBL:CHEMBL588683 ? unclear Mechanistic
CHEMBL:CHEMBL593254 ? unclear Mechanistic
CHEMBL:CHEMBL588525 ? unclear Mechanistic
PURPURIN ? unclear Mechanistic
CHEMBL:CHEMBL316796 ? unclear Mechanistic

Showing top 40 of 283 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
CARBOPLATIN ? unclear Mechanistic
OLAPARIB ? unclear Mechanistic
TALAZOPARIB ? unclear Mechanistic
NIRAPARIB ? unclear Mechanistic
RUCAPARIB ? unclear Mechanistic
QUARFLOXIN ? unclear Mechanistic
CISPLATIN ? unclear Mechanistic
VELIPARIB ? unclear Mechanistic
BOSUTINIB ? unclear Mechanistic
PLATINUM COMPOUND ? unclear Mechanistic
TEMOZOLOMIDE ? unclear Mechanistic
ENZALUTAMIDE ? unclear Mechanistic
DASATINIB ANHYDROUS ? unclear Mechanistic
GEMCITABINE ? unclear Mechanistic
PIDNARULEX ? unclear Mechanistic
SACITUZUMAB GOVITECAN ? unclear Mechanistic
CEDIRANIB ? unclear Mechanistic
INIPARIB ? unclear Mechanistic
PARP/TANKYRASE INHIBITOR 2X-121 ? unclear Mechanistic
Therapeutic Agent Effect Direction Evidence Tier Potency Source
ABEMACICLIB ↓ inhibits Mechanistic
TRILACICLIB ↓ inhibits Mechanistic
CDK2 INHIBITOR IV ↓ inhibits Mechanistic
VORUCICLIB ↓ inhibits Mechanistic
LEROCICLIB ↓ inhibits Mechanistic
RIVICICLIB ↓ inhibits Mechanistic
CDK INHIBITOR 4.35 ↓ inhibits Mechanistic
AZD5438 ↓ inhibits Mechanistic
RIBOCICLIB SUCCINATE ? unclear Mechanistic
ALPELISIB ? unclear Mechanistic
ALVOCIDIB ↓ inhibits Mechanistic
CDK4 INHIBITOR III ↓ inhibits Mechanistic
PURVALANOL B ↓ inhibits Mechanistic
PHA-793887 ? unclear Mechanistic
RONICICLIB ↓ inhibits Mechanistic
MILCICLIB ↓ inhibits Mechanistic
R547 ↓ inhibits Mechanistic
ASCORBIC ACID ? unclear Mechanistic
RGB-286638 ↓ inhibits Mechanistic
ANTINEOPLASTIC AGENT ? unclear Mechanistic
CGP74514A ↓ inhibits Mechanistic
APREMILAST ? unclear Mechanistic
CROZBACICLIB ↓ inhibits Mechanistic
EBVACICLIB ↓ inhibits Mechanistic
VUSTANACICLIB ↓ inhibits Mechanistic
CIMPUCICLIB ↓ inhibits Mechanistic
PURVALANOL A ↓ inhibits Mechanistic
BSJ-03-123 ↓ inhibits Mechanistic
CDK1/2/4 INHIBITOR AG-024322 ? unclear Mechanistic
TANUXICICLIB ↓ inhibits Mechanistic
TIBREMCICLIB ↓ inhibits Mechanistic
BIREOCICLIB ↓ inhibits Mechanistic
RECOMBINANT TRANSFORMING GROWTH FACTOR ? unclear Mechanistic
BSJ-04-132 ↓ inhibits Mechanistic
BSJ-03-204 ↓ inhibits Mechanistic
CP-10 ↓ inhibits Mechanistic
COMPOUND 9B [PMID: 18986805] ↓ inhibits Mechanistic
NICOTINE POLACRILEX ? unclear Mechanistic
DEXAMETHASONE ? unclear Mechanistic
SU9516 ↓ inhibits Mechanistic

Showing top 40 of 255 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
TRILACICLIB ↓ inhibits Mechanistic
INIXACICLIB ↓ inhibits Mechanistic
CDK/CRK INHIBITOR ↓ inhibits Mechanistic
VUSTANACICLIB ↓ inhibits Mechanistic
PALBOCICLIB ↓ inhibits Mechanistic 16.0 nM (IC50)
TANUXICICLIB ↓ inhibits Mechanistic
FULVESTRANT ? unclear Mechanistic
CIMPUCICLIB ↓ inhibits Mechanistic
PHA-793887 ↓ inhibits Mechanistic
ABEMACICLIB ↓ inhibits Mechanistic
TRILACICLIB DIHYDROCHLORIDE ↓ inhibits Mechanistic
ATIRMOCICLIB ↓ inhibits Mechanistic
RIBOCICLIB SUCCINATE ? unclear Mechanistic
NARAZACICLIB ↓ inhibits Mechanistic
LEROCICLIB ↓ inhibits Mechanistic
AZD5438 ↓ inhibits Mechanistic
RGB-286638 ↓ inhibits Mechanistic
UCN-01 ↓ inhibits Mechanistic
BSJ-03-123 ↓ inhibits Mechanistic
ULECACICLIB ↓ inhibits Mechanistic
BIREOCICLIB ↓ inhibits Mechanistic
CROZBACICLIB ↓ inhibits Mechanistic
EBVACICLIB ↓ inhibits Mechanistic
APREMILAST ? unclear Mechanistic
CP-10 ↓ inhibits Mechanistic
PRT3645 ↓ inhibits Mechanistic
CULMERCICLIB ↓ inhibits Mechanistic
TIBREMCICLIB ↓ inhibits Mechanistic
ALVOCIDIB ↓ inhibits Mechanistic 80.0 nM (IC50)
RIBOCICLIB ↓ inhibits Mechanistic 39.0 nM (IC50)
AT-7519 ↓ inhibits Mechanistic
BSJ-03-204 ↓ inhibits Mechanistic
RONICICLIB ↓ inhibits Mechanistic
BSJ-04-132 ↓ inhibits Mechanistic
VORUCICLIB ↓ inhibits Mechanistic
DALPICICLIB ↓ inhibits Mechanistic
AZD-5438 ? unclear Mechanistic
FISETIN ↓ inhibits Mechanistic 850.0 nM (IC50)
APIGENIN ↓ inhibits Mechanistic 1700.0 nM (IC50)
KAEMPFEROL ↓ inhibits Mechanistic 22000.0 nM (IC50)

Showing top 40 of 226 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
TYRPHOSTIN AG 879 ? unclear Mechanistic
TAK-285 ↓ inhibits Mechanistic
PERTUZUMAB ↓ inhibits Mechanistic
SAPITINIB ↓ inhibits Mechanistic
CANERTINIB ↓ inhibits Mechanistic 529.0 nM (IC50)
LAPATINIB ↓ inhibits Mechanistic 9.0 nM (IC50)
AFATINIB DIMALEATE ↓ inhibits Mechanistic
MUBRITINIB ↓ inhibits Mechanistic
JNJ-26483327 ↓ inhibits Mechanistic
NAKIJIQUINONE I ? unclear Mechanistic
AEE788 ↓ inhibits Mechanistic
HEMAY-022 ↓ inhibits Mechanistic
MM-111 ? unclear Mechanistic
NERATINIB ↓ inhibits Mechanistic
DACOMITINIB ANHYDROUS ↓ inhibits Mechanistic
IXABEPILONE ? unclear Mechanistic
DIETHYLSTILBESTROL ? unclear Mechanistic
TAMATINIB ? unclear Mechanistic
S-222611 ↓ inhibits Mechanistic
CP-724714 ? unclear Mechanistic
AKT INHIBITOR MK2206 ? unclear Mechanistic
ANTINEOPLASTIC AGENT ? unclear Mechanistic
TIPIFARNIB ? unclear Mechanistic
BMS-599626 ↓ inhibits Mechanistic
MIFANERTINIB ↓ inhibits Mechanistic
GEFITINIB ↓ inhibits Mechanistic 1604.0 nM (IC50)
ADO-TRASTUZUMAB EMTANSINE ? unclear Mechanistic
CARBOPLATIN ? unclear Mechanistic
TRASTUZUMAB DUOCARMAZINE ~ modulates Mechanistic
POZIOTINIB ↓ inhibits Mechanistic
HLX22 ? unclear Mechanistic
CURCUMIN ? unclear Mechanistic
HSP90 INHIBITOR ? unclear Mechanistic
TUCATINIB ↓ inhibits Mechanistic
TRASTUZUMAB ↓ inhibits Mechanistic
EPIGALLOCATECHIN GALLATE ? unclear Mechanistic
PACLITAXEL PROTEIN-BOUND ? unclear Mechanistic
FAM-TRASTUZUMAB DERUXTECAN-NXKI ? unclear Mechanistic
DASATINIB ANHYDROUS ? unclear Mechanistic
TRASTUZUMAB EMTANSINE ~ modulates Mechanistic

Showing top 40 of 336 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
ESTRONE ↑ activates Mechanistic 480.0 nM (EC50)
EVEROLIMUS ? unclear Mechanistic
ANASTROZOLE ? unclear Mechanistic
SIVIFENE ? unclear Mechanistic
ARZOXIFENE ~ modulates Mechanistic
ENDOXIFEN ↓ inhibits Mechanistic
OSPEMIFENE ↓ inhibits Mechanistic
RALOXIFEN ? unclear Mechanistic
FULVESTRANT ↓ inhibits Mechanistic 6.0 nM (IC50)
INAVOLISIB ? unclear Mechanistic
TESTOSTERONE PROPIONATE ? unclear Mechanistic
PHENYLMERCURIC ACETATE ? unclear Mechanistic
ESTRADIOL CYPIONATE ↑ activates Mechanistic
ESTROGEN ? unclear Mechanistic
METHOXSALEN ? unclear Mechanistic
BORIC ACID ? unclear Mechanistic
IMLUNESTRANT ↓ inhibits Mechanistic
PROTOAPIGENONE ? unclear Mechanistic
CLOMIPHENE CITRATE ? unclear Mechanistic
DAUNORUBICIN HYDROCHLORIDE ? unclear Mechanistic
NERATINIB ? unclear Mechanistic
ALACHLOR ? unclear Mechanistic
METHAMPHETAMINE ? unclear Mechanistic
OCHRATOXIN A ? unclear Mechanistic
CETRIMONIUM BROMIDE ? unclear Mechanistic
EXEMESTANE ? unclear Mechanistic
GW7647 ? unclear Mechanistic
NORGESTREL ? unclear Mechanistic
AMCENESTRANT ↓ inhibits Mechanistic
LETROZOLE ? unclear Mechanistic
PROGESTERONE ? unclear Mechanistic
DIETHYLSTILBESTROL ↑ activates Mechanistic 12.0 nM (EC50)
ESTRIOL ↑ activates Mechanistic
16&ALPHA;-HYDROXYESTRONE ↑ activates Mechanistic
BRILANESTRANT ? unclear Mechanistic
LEVONORGESTREL ? unclear Mechanistic
ACOLBIFENE ? unclear Mechanistic
PROPYLPYRAZOLETRIOL ↑ activates Mechanistic
ESTRADIOL VALERATE ↑ activates Mechanistic
MEGESTROL ? unclear Mechanistic

Showing top 40 of 386 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
NIRAPARIB ↓ inhibits Mechanistic
VELIPARIB ↓ inhibits Mechanistic
4-[3-(1,4-DIAZEPAN-1-YLCARBONYL)-4-FLUOROBENZYL]PHTHALAZIN-1(2H)-ONE ↓ inhibits Mechanistic
PAMIPARIB ↓ inhibits Mechanistic
OLAPARIB ↓ inhibits Mechanistic
COMPOUND 5 [TOMASSI ET AL., 2020] ↓ inhibits Mechanistic
COMPOUND 9 [LIN ET AL., 2023] ↓ inhibits Mechanistic
INIPARIB ↓ inhibits Mechanistic
AZ1366 ↓ inhibits Mechanistic
DUAL VEGFR/PARP INHIBITOR 14B ↓ inhibits Mechanistic
NIACIN ? unclear Mechanistic
2X-121 ↓ inhibits Mechanistic
AMELPARIB DIHYDROCHLORIDE DIHYDRATE ↓ inhibits Mechanistic
CEP-9722 ? unclear Mechanistic
ORAL AZACITIDINE ? unclear Mechanistic
RUCAPARIB PHOSPHATE ↓ inhibits Mechanistic
AG14361 ↓ inhibits Mechanistic
ME0328 ↓ inhibits Mechanistic
SARUPARIB ↓ inhibits Mechanistic
SENAPARIB ↓ inhibits Mechanistic
NIRAPARIB TOSYLATE ? unclear Mechanistic
TALAZOPARIB ↓ inhibits Mechanistic
PJ34 ↓ inhibits Mechanistic
TALAZOPARIB TOSYLATE ↓ inhibits Mechanistic
PARP1 INHIBITOR (S)-G9 ↓ inhibits Mechanistic
NICARAVEN ? unclear Mechanistic
PARP-1/2 INHIBITOR ABT-767 ? unclear Mechanistic
INO-1001 ? unclear Mechanistic
BGP-15 ? unclear Mechanistic
RUCAPARIB ↓ inhibits Mechanistic
TRABECTEDIN ? unclear Mechanistic
VENADAPARIB ↓ inhibits Mechanistic
FLUZOPARIB ↓ inhibits Mechanistic
MC2050 ↓ inhibits Mechanistic
PARP INHIBITOR E7016 ? unclear Mechanistic
LERZEPARIB ↓ inhibits Mechanistic
CICLOPIROX ↓ inhibits Mechanistic
E-7016 ↓ inhibits Mechanistic
RUCAPARIB CAMSYLATE ↓ inhibits Mechanistic
PALACAPARIB ↓ inhibits Mechanistic

Showing top 40 of 207 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
ETHYNODIOL DIACETATE ↑ activates Mechanistic
MIFEPRISTONE ↓ inhibits Mechanistic 0.028 nM (IC50)
LAPATINIB ? unclear Mechanistic
ETONOGESTREL ↑ activates Mechanistic
GESTODENE ↑ activates Mechanistic
DOCETAXEL ANHYDROUS ? unclear Mechanistic
PROGESTERONE ↑ activates Mechanistic 2.9 nM (EC50)
NERATINIB ? unclear Mechanistic
NORELGESTROMIN ↑ activates Mechanistic
ZK112993 ↓ inhibits Mechanistic
ASOPRISNIL ↓ inhibits Mechanistic
NORGESTIMATE ↑ activates Mechanistic
TELAPRISTONE ? unclear Mechanistic
CYPROTERONE ACETATE ↑ activates Mechanistic
CHLORMADINONE ACETATE ~ modulates Mechanistic
TAMOXIFEN ? unclear Mechanistic
EXEMESTANE ? unclear Mechanistic
PERTUZUMAB ? unclear Mechanistic
PROGESTIN ? unclear Mechanistic
MEGESTROL ACETATE ↑ activates Mechanistic
PROGESTOGEN ? unclear Mechanistic
LONAPRISAN ↓ inhibits Mechanistic
NORGESTREL ↑ activates Mechanistic
NOMEGESTROL ↑ activates Mechanistic
MEDROXYPROGESTERONE ACETATE ↑ activates Mechanistic 0.15 nM (EC50)
ULIPRISTAL ~ modulates Mechanistic
DYDROGESTERONE ↑ activates Mechanistic
NORETHYNODREL ↑ activates Mechanistic
ERIBULIN ? unclear Mechanistic
ESTRADIOL VALERATE/DIENOGEST ? unclear Mechanistic
NORETHINDRONE ACETATE ↑ activates Mechanistic
PROMEGESTONE ↑ activates Mechanistic
CHEMBL:CHEMBL2059711 ? unclear Mechanistic
LETROZOLE ? unclear Mechanistic
DANAZOL ↑ activates Mechanistic
ULIPRISTAL ACETATE ↓ inhibits Mechanistic
APR19 ↓ inhibits Mechanistic
PALBOCICLIB ? unclear Mechanistic
PF-05019702 ↓ inhibits Mechanistic
VILAPRISAN ? unclear Mechanistic

Showing top 40 of 158 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
SURAMIN ? unclear Mechanistic
TEMSIROLIMUS ? unclear Mechanistic
RIGOSERTIB ↓ inhibits Mechanistic
NEOLYMPHOSTIN A ↓ inhibits Mechanistic
INAVOLISIB ↓ inhibits Mechanistic
RIGOSERTIB SODIUM ? unclear Mechanistic
TAK-733 ? unclear Mechanistic
APILIMOD DIMESYLATE CAPSULE ? unclear Mechanistic
COMPOUND 15A [PMID: 32069401] ↓ inhibits Mechanistic
COMPOUND 41 [PMID: 31855425] ↓ inhibits Mechanistic
ERDAFITINIB ? unclear Mechanistic
RIBOCICLIB ? unclear Mechanistic
BRAFV600/PI3K INHIBITOR ASN003 ? unclear Mechanistic
GSK2636771 ↓ inhibits Mechanistic
ZINC SULFATE ANHYDROUS ? unclear Mechanistic
EVEROLIMUS ? unclear Mechanistic
COPANLISIB ↓ inhibits Mechanistic
TANESPIMYCIN ? unclear Mechanistic
CAPIVASERTIB ? unclear Mechanistic
SAMOTOLISIB ↓ inhibits Mechanistic
COPANLISIB HYDROCHLORIDE ↓ inhibits Mechanistic
PAXALISIB ↓ inhibits Mechanistic
U0126 ? unclear Mechanistic
PILARALISIB ↓ inhibits Mechanistic
M-2698 ? unclear Mechanistic
GSK2334470 ? unclear Mechanistic
BIMIRALISIB ↓ inhibits Mechanistic
PALBOCICLIB ? unclear Mechanistic
SONOLISIB ↓ inhibits Mechanistic 88.0 nM (IC50)
VULOLISIB ↓ inhibits Mechanistic
ALPELISIB ↓ inhibits Mechanistic
DOCETAXEL ANHYDROUS ? unclear Mechanistic
COMPOUND 27 [PMID: 35834807] ↓ inhibits Mechanistic
MILTEFOSINE ? unclear Mechanistic
CARBOPLATIN ? unclear Mechanistic
ACALISIB ↓ inhibits Mechanistic
GEDATOLISIB ↓ inhibits Mechanistic
VS-5584 ↓ inhibits Mechanistic
XRD-0394 ↓ inhibits Mechanistic
IZORLISIB ? unclear Mechanistic

Showing top 40 of 444 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
SACITUZUMAB GOVITECAN ? unclear Mechanistic
DATOPOTAMAB DERUXTECAN ~ modulates Mechanistic
HIMB1636-MMAE ? unclear Mechanistic
SACITUZUMAB TIRUMOTECAN ? unclear Mechanistic
Therapeutic Agent Effect Direction Evidence Tier Potency Source
FLUOROURACIL ? unclear Mechanistic
DAUNORUBICIN HYDROCHLORIDE ? unclear Mechanistic
VOSAROXIN ↓ inhibits Mechanistic
EPIRUBICIN ? unclear Mechanistic
KAEMPFERITRIN ? unclear Mechanistic
MAKALUVAMINE E ? unclear Mechanistic
ALDOXORUBICIN ↓ inhibits Mechanistic
CHEMBL:CHEMBL244268 ? unclear Mechanistic
PYRAZOLOACRIDINE ? unclear Mechanistic
ACRIDINE CARBOXAMIDE ? unclear Mechanistic
BETULIN ? unclear Mechanistic 38600.0 nM (IC50)
CHEMBL:CHEMBL596082 ? unclear Mechanistic
LOMEFLOXACIN ? unclear Mechanistic
CHEMBL:CHEMBL1080077 ? unclear Mechanistic
DOXORUBICIN-MAGNETIC TARGETED CARRIER COMPLEX ? unclear Mechanistic
GENISTEIN ? unclear Mechanistic
ROSOXACIN ? unclear Mechanistic
DOXORUBICIN-HPMA CONJUGATE ? unclear Mechanistic
PODOFILOX ? unclear Mechanistic
MITOXANTRONE HYDROCHLORIDE ↓ inhibits Mechanistic
PIXANTRONE ? unclear Mechanistic
TRICITRINOL B ? unclear Mechanistic
FRANGULIN B ? unclear Mechanistic
FLUOROQUINOLONE ANTIBIOTIC ? unclear Mechanistic
LYCOBETAINE ? unclear Mechanistic
MAKALUVAMINE C TFA SALT ? unclear Mechanistic
TAS-103 ? unclear Mechanistic
AMSACRINE ↓ inhibits Mechanistic 9940.0 nM (IC50)
QUERCETIN ? unclear Mechanistic
C-1311 ↓ inhibits Mechanistic
ANTHRACYCLINE ANTINEOPLASTIC ANTIBIOTIC ? unclear Mechanistic
DAUNORUBICIN LIPOSOMAL ↓ inhibits Mechanistic
IDARUBICIN ? unclear Mechanistic
OLEANDEROLIDE ? unclear Mechanistic
CHEMBL:CHEMBL594259 ? unclear Mechanistic
NEMORUBICIN ? unclear Mechanistic
CHEMBL:CHEMBL594153 ? unclear Mechanistic
DANIQUIDONE ? unclear Mechanistic
ELSAMITRUCIN ? unclear Mechanistic
VALRUBICIN ? unclear Mechanistic

Showing top 40 of 289 agents ranked by evidence tier.


Clinical Trials

Drug, biologic and supplement trials (treatment or prevention) from ClinicalTrials.gov whose main condition is Breast Cancer: recruiting, active or completed, most recently updated first. Data retrieved 2026-10-28.

NCT04134598 Phase: 3 Started: 2021-02-08

Rationale and relevance for patients and the scientific community. In low risk early stage patients ≥70 years, exclusive radiation therapy (RT) approach might be superior in terms of Health-Related Quality of Life (HRQoL), when compared to exclusive endocrine therapy (ET) following breast-conserving...

NCT07900516 Phase: 2 Started: 2026-08-01

To explore the efficacy and safety of Culmerciclib combined with chemotherapy as neoadjuvant therapy for HR+/HER2- breast cancer patients who are insensitive to neoadjuvant TAC (docetaxel, doxorubicin, cyclophosphamide) chemotherapy.

NCT07391774 Phase: 3 Started: 2026-08-10

This phase III trial compares standard of care hormone therapy plus ribociclib to chemotherapy followed by hormone therapy plus ribociclib for the treatment of patients with high anatomic stage breast cancer with low risk of the cancer returning (low risk recurrence). Ribociclib may stop the growth ...

NCT03025035 Phase: 2 Started: 2017-09-10

This trial will evaluate the use of immunotherapy and PARP inhibition in a population with incurable advanced breast cancer associated with a germline BRCA mutation or HDR-defect. The main objective is to examine overall response rate of pembrolizumab (immunotherapy) in combination with Olaparib (PA...

NCT06908928 Phase: 1 Started: 2025-08-11

The goal of this clinical trial is to investigate if treatment with bulumtatug fuvedotin is effective in triple-negative breast cancer patients who have previously received treatment with an antibody-drug conjugates.

NCT07109726 Phase: 1/2 Started: 2025-09-23

This is a Phase 1/2, open-label, multicenter study evaluating the safety, tolerability, pharmacokinetics, pharmacodynamics and anti-tumor activity of TER-2013 in patients with advanced solid tumors harboring AKT/PI3K/PTEN pathway alterations.

NCT06324357 Phase: 1/2 Started: 2024-06-28

This study is open to adults aged 18 years and older with different types of HER2+ cancer that has spread and cannot be removed by surgery. People can take part in this study if their tumours show HER2 aberrations and previous treatment was not successful. The purpose of this study is to find a suit...

NCT06058377 Phase: 3 Started: 2023-11-27

This phase III trial compares the addition of an immunotherapy drug (durvalumab) to usual chemotherapy versus usual chemotherapy alone in treating patients with MammaPrint High 2 Risk (MP2) stage II-III hormone receptor positive, HER2 negative breast cancer. Immunotherapy with monoclonal antibodies,...

NCT06188520 Phase: 1/2 Started: 2023-12-05

This study is designed to evaluate AZD8421 alone and in combination with selected targeted anti-cancer drugs in patients with ER+HER2- advanced breast cancer, and patients with metastatic high-grade serious ovarian cancer.

NCT06144944 Phase: 3 Started: 2024-01-17

This is a multi-center, open-lable, prospective, randomized phase III clinical trial to further validate the efficacy and safety of neoadjuvant pyrotinib combined with chemotherapy in HR-positive/HER2-low (IHC 2+/FISH-negative) high-risk early breast cancer

NCT06891833 Phase: 2/3 Started: 2025-06-05

This trial is a registered phase III, randomized, open and multicenter study to evaluate the efficacy and safety of BL-M07D1 with or without Pertuzumab in the neoadjuvant treatment of HER2-positive breast cancer. The study is divided into a single-arm study phase (Phase II) and a randomized controll...

NCT07896668 Phase: 2 Started: 2025-09-01

A prospective, multicenter, single-arm clinical study enrolling patients with histologically confirmed invasive carcinoma, clinical stage II-III, known PD-L1 status, and treatment-naïve triple-negative breast cancer. Patients will receive neoadjuvant therapy with pucotenlimab, anlotinib, and nab-pac...

NCT05646862 Phase: 3 Started: 2023-06-07

This is a Phase III, multicenter, randomized, open-label, global study designed to evaluate the efficacy and safety of inavolisib plus fulvestrant compared with alpelisib plus fulvestrant in patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2) -negative, PIK3...

NCT07134153 Phase: 1/2 Started: 2025-05-12

Multiple trials confirm systemic T-DXd efficacy in HER2+ breast cancer with leptomeningeal/brain metastases, yet median LM survival remains 3-4 months, highlighting unmet needs. While systemic therapies improve survival, intracranial disease control remains limited due to poor BBB penetration. Precl...

NCT07054190 Phase: 2 Started: 2025-09-09

This study will evaluate the safety and efficacy of inavolisib combination therapies in participants with untreated, PIK3CA-mutated, Stage II-III, estrogen receptor (ER)-positive, Human Epidermal Growth Factor Receptor 2 (HER2)-negative breast cancer (BC).


Agents Found By Disease-Level Search

Searched directly from “Breast Cancer” via ClinicalTrials.gov interventions and Open Targets' disease→drug data — independent of the 13-gene target panel above. This surfaces agents whose mechanism doesn't route through a curated gene (combination therapies, standard-of-care drugs, targets outside the panel).

44 agents shown (approved or with trial evidence) — 28 not found by the gene-target search above.

DocetaxelNOT in gene-target list

Approved · 4 trials · source: ClinicalTrials.gov, Open Targets
NCT00391092 NCT01779206 NCT00003565

CyclophosphamideNOT in gene-target list

Phase 3 · 4 trials · source: ClinicalTrials.gov, Open Targets
NCT05269381 NCT01779206 NCT02276300

Fulvestrant

Approved · 4 trials · source: ClinicalTrials.gov, Open Targets
NCT03344536 NCT03691493 NCT03280563

Pembrolizumab

Phase 3 · 3 trials · source: ClinicalTrials.gov, Open Targets
NCT02432963 NCT05269381 NCT07341867

Epirubicin

Phase 3 · 2 trials · source: ClinicalTrials.gov, Open Targets
NCT00193206 NCT01779206

SargramostimNOT in gene-target list

Phase 3 · 2 trials · source: ClinicalTrials.gov, Open Targets
NCT05269381 NCT02276300

Exemestane

Approved · 2 trials · source: ClinicalTrials.gov, Open Targets
NCT03691493 NCT03280563

Tamoxifen

Approved · 2 trials · source: ClinicalTrials.gov, Open Targets
NCT03691493 NCT03280563

Bevacizumab

Approved · 2 trials · source: ClinicalTrials.gov, Open Targets
NCT06307249 NCT03280563

adjuvant therapyNOT in gene-target list

· 2 trials · source: ClinicalTrials.gov
NCT00667121 NCT00054301

Abemaciclib

Approved · 2 trials · source: ClinicalTrials.gov, Open Targets
NCT05095207 NCT03280563

PaclitaxelNOT in gene-target list

Approved · 2 trials · source: ClinicalTrials.gov, Open Targets
NCT01779206 NCT07341867

carboplatin

Phase 3 · 2 trials · source: ClinicalTrials.gov, Open Targets
NCT00005963 NCT07341867

bevacizumab [Avastin]NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00391092

HerceptinNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00391092

ICG-SG incubation solutionNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT05708144

Modified Vaccinia Virus Ankara Vaccine Expressing p53NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02432963

Gemcitabine

Phase 3 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT00193206

Albumin-bound PaclitaxelNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00193206

MBCT-SNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT04472104

SexEdNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT04472104

TREATMENT GROUP(QL1706 + anlotinib+ nab-paclitaxel )NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT07601178

RuxolitinibNOT in gene-target list

Phase 2 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT02066532

Trastuzumab

Approved · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT02066532

NIR-II probe (i.e ICG-CK) incubation solutionNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT07154563

ZoladexNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01712893

Tailored reminder letterNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT07472036

Gefitinib

Phase 2 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT00357734

ChlorhexidineNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02479347

Povidone-IodineNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02479347

Neoantigen Peptide VaccineNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT05269381

Computed TomographyNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT05269381

Debio 1347NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03344536

AprepitantNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01298193

Anastrozole

Approved · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT03691493

Letrozole

Approved · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT03691493

Palbociclib

Approved · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT03691493

SNPNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT06307249

Palbociclib 125mgNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT06307249

citalopram hydrobromideNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00667121

escitalopram oxalateNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00667121

gabapentinNOT in gene-target list

Phase 3 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT00667121

sertraline hydrochloride

· 1 trial · source: ClinicalTrials.gov
NCT00667121

tamoxifen citrate

Approved · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT00667121

Generated by the Open Source Medicine Foundation Biomarker Pipeline — 2026-10-08. Data sources: DGIdb, Open Targets, ChEMBL, PubMed, ClinicalTrials.gov. Not medical advice.