Science - USA (2022-01-14)

Fasslet al.,Science 375 , eabc1495 (2022) 14 January 2022 13 of 19

Additional target Inhibitor Immune

checkpoint

inhibitor

Tumor

type

Trial identifier

............................................................................................................................................................................................................................................................................................................................................

FGFR1-3............................................................................................................................................................................................................................................................................................................................................Rogaratinib FGFR1-3+/HR+breast cancer NCT04483505

IGF-1R............................................................................................................................................................................................................................................................................................................................................Ganitumab Ewing sarcoma NCT04129151

VEGF1-3 receptors +

PD-L1

Axitinib Avelumab NSCLC NCT03386929

............................................................................................................................................................................................................................................................................................................................................

RAF............................................................................................................................................................................................................................................................................................................................................Sorafenib Leukemia NCT03132454

MEK PD-0325901,

binimetinib

KRAS mutant NSCLC, TNBC,

KRAS and NRAS mutant

metastatic or unresectable

colorectal cancer

NCT02022982, NCT03170206,

NCT04494958, NCT03981614

............................................................................................................................................................................................................................................................................................................................................

ERK Ulixertinib Advanced pancreatic cancer

and other solid tumors

NCT03454035

............................................................................................................................................................................................................................................................................................................................................

PI3K............................................................................................................................................................................................................................................................................................................................................Copanlisib HR+breast cancer NCT03128619

PI3K Taselisib, pictilisib,

GDC-0077

PIK3CA mutant advanced solid

tumors, PIK3CA mutant and

HR+breast cancer

NCT02389842, NCT04191499,

NCT03006172

............................................................................................................................................................................................................................................................................................................................................

PI3K/mTOR Gedatolisib Metastatic breast cancer,

advanced squamous cell lung,

pancreatic, head and neck

cancer and other solid tumors

NCT02684032, NCT03065062,

NCT02626507

............................................................................................................................................................................................................................................................................................................................................

mTOR............................................................................................................................................................................................................................................................................................................................................Everolimus, vistusertib HR+breast cancer NCT02871791

AKT Ipatasertib HR+breast cancer, metastatic

breast cancer, metastatic

gastrointestinal tumors,

NSCLC

NCT03959891, NCT04060862,

NCT04591431

............................................................................................................................................................................................................................................................................................................................................

BTK............................................................................................................................................................................................................................................................................................................................................Ibrutinib Mantle cell lymphoma NCT03478514

BCL-2 Venetoclax ER+/BCL-2+advanced

or metastatic breast

cancer

NCT03900884

............................................................................................................................................................................................................................................................................................................................................

AR............................................................................................................................................................................................................................................................................................................................................AR antagonists: bicalutamide AR+metastatic breast cancer NCT02605486

Lysosome +

aromatase

Hydroxychloroquine + letrozole ER+breast cancer NCT03774472

............................................................................................................................................................................................................................................................................................................................................

Proliferating cells............................................................................................................................................................................................................................................................................................................................................Standard chemotherapy Stage IV ER+breast cancer NCT03355157

Proliferating cells Radiation Stage IV ER+breast cancer NCT03870919,

NCT03691493,

............................................................................................................................................................................................................................................................................................................................................NCT04605562

BCR-ABL............................................................................................................................................................................................................................................................................................................................................Bosutinib HR+breast cancer NCT03854903

Ribociclib

............................................................................................................................................................................................................................................................................................................................................

Aromatase Letrozole, anastrozole,

exemestane

HR+breast cancer,

metastatic breast

cancer, ovarian

cancer

NCT04256941, NCT03425838,

NCT03822468, NCT02712723,

NCT03673124, NCT02941926,

NCT03248427, NCT03671330,

NCT02333370, NCT01958021,

............................................................................................................................................................................................................................................................................................................................................NCT03425838

LHRH LHRH agonists:

goserelin, leuprolide

HR+breast cancer NCT03944434

............................................................................................................................................................................................................................................................................................................................................

ER ER antagonists: fulvestrant HR+breast cancer,

advanced breast cancer

NCT03227328, NCT02632045,

............................................................................................................................................................................................................................................................................................................................................NCT02632045, NCT03555877

PD-1 Spartalizumab Breast cancer and ovarian

cancer, recurrent and/or

metastatic head and neck

squamous cell carcinoma,

melanoma

NCT03294694, NCT04213404,

NCT03484923

............................................................................................................................................................................................................................................................................................................................................

HER2 Trastuzumab, pertuzumab,

T-DM1

HER2+breast cancer NCT03913234, NCT02657343

............................................................................................................................................................................................................................................................................................................................................

EGFR............................................................................................................................................................................................................................................................................................................................................Nazartinib (EGF816) EGFR mutant NSCLC NCT03333343

RAF Encorafenib, LXH254 NSCLC, BRAF

mutant melanoma

NCT02974725, NCT03333343,

............................................................................................................................................................................................................................................................................................................................................NCT04417621, NCT02159066

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