Science - USA (2022-01-14)

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

Additional target Inhibitor Immune

checkpoint

inhibitor

Tumor

type

Trial identifier

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

MEK Binimetinib BRAF V600-dependent

advanced solid tumors,

melanoma

NCT01543698, NCT02159066

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

PI3K Alpelisib Breast cancer with

PIK3CA mutation

NCT03439046

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

mTOR Everolimus Advanced dedifferentiated

liposarcoma, leiomyosarcoma,

glioma, astrocytoma,

glioblastoma, endometrial

carcinoma, pancreatic cancer,

neuroendocrine tumors

NCT03114527, NCT03355794,

NCT03834740, NCT03008408,

NCT02985125, NCT03070301

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

mTOR + inflammation............................................................................................................................................................................................................................................................................................................................................Everolimus + dexamethasone ALL NCT03740334

SHP2............................................................................................................................................................................................................................................................................................................................................TNO155 Advanced solid tumors NCT04000529

AR AR antagonists:

bicalutamide,

enzalutamide

TNBC, metastatic

prostate carcinoma

NCT03090165, NCT02555189

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

HDAC............................................................................................................................................................................................................................................................................................................................................Belinostat TNBC, ovarian cancer NCT04315233

proliferating cells Standard chemotherapy Ovarian cancer, metastatic

solid tumors, soft tissue

sarcoma, hepatocellular

carcinoma

NCT03056833, NCT03237390,

NCT03009201, NCT02524119

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

Abemaciclib

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

Aromatase Letrozole, anastrozole,

exemestane

HR+breast cancer,

metastatic breast

cancer, endometrial

cancer

NCT04256941, NCT03425838,

NCT04227327, NCT04393285,

NCT04305236, NCT03643510,

NCT03675893, NCT04352777,

............................................................................................................................................................................................................................................................................................................................................NCT04293393, NCT02057133

ER ER antagonists: fulvestrant Advanced breast cancer,

low-grade serous ovarian cancer

NCT03227328, NCT03531645,

............................................................................................................................................................................................................................................................................................................................................NCT04158362, NCT01394016

PD-1 Nivolumab,

pembrolizumab

Head and neck cancer,

gastroesophageal cancer,

NSCLC, HR+breast cancer

NCT04169074, NCT03655444,

NCT03997448, NCT02779751

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

ER + PD-L1 ER antagonists: fulvestrant Atezolizumab HR+breast cancer, metastatic

breast cancer

NCT03280563

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

AKT + ER + PD-L1 Ipatasertib + ER

antagonists: fulvestrant

Atezolizumab HR+breast cancer NCT03280563

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

PD-L1............................................................................................................................................................................................................................................................................................................................................LY3300054 Advanced solid tumors NCT02791334

HER2 Trastuzumab HER2+metastatic

breast cancer

NCT04351230

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

Receptor tyrosine

kinases

Sunitinib Metastatic renal

cell carcinoma

NCT03905889

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

IGF-1/IGF-2............................................................................................................................................................................................................................................................................................................................................Xentuzumab HR+breast cancer NCT03099174

VEGF-A............................................................................................................................................................................................................................................................................................................................................Bevacizumab Glioblastoma NCT04074785

PI3K Copanlisib HR+breast cancer, metastatic

breast cancer

NCT03939897

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

PI3K/mTOR............................................................................................................................................................................................................................................................................................................................................LY3023414 Metastatic cancer NCT01655225

ERK1/2 LY3214996 tumors with ERK1/2

mutations, glioblastoma,

metastatic cancer

NCT04534283, NCT04391595,

NCT02857270

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

Trilaciclib

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

Proliferating cells Chemotherapy SCLC: This trial evaluates the

potential clinical benefit of

trilaciclib in preventing

chemotherapy-induced

myelosuppression in patients

receiving chemotherapy

NCT04504513

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

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