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DRUG CLASS:

Angiopoietin 2 inhibitor

5d
A study of the safety, efficacy, and cost-effectiveness of using non-vitrectomised subretinal anti-VEGF injections to treat neovascular age-related macular degeneration (ChiCTR2400090827)
P1, N=80, Not yet recruiting, Department of Ophthalmology and Visual Sciences, CUHK; Department of Ophthalmology and Visual Sciences, The Chinese University of Hong Kong
New P1 trial • HEOR • Cost effectiveness
7d
New trial • Real-world evidence • Real-world
25d
USP9X-enriched MSC-sEV inhibits LSEC angiogenesis in MASH mice by downregulating the IκBα/NF-κB/Ang-2 pathway. (PubMed, Pharmacol Res)
Knockdown of USP9X attenuated the regulatory effects of MSC-sEV on Ang-2 expression, LSEC angiogenesis, and the progression of MASH. In conclusion, our findings indicate that USP9X delivered via MSC-sEV can suppress LSEC angiogenesis and alleviate MASH-induced liver fibrosis through the IκBα/NF-κB/Ang-2 signaling pathway.
Preclinical • Journal
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NFKBIA (NFKB Inhibitor Alpha 2) • USP9X (Ubiquitin Specific Peptidase 9 X-Linked)
1m
Trial completion
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PD-L1 (Programmed death ligand 1)
|
PD-L1 expression
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ezabenlimab (BI 754091) • BI 836880
1m
Trial completion
2ms
A Phase 1 Trial of Trebananib, an Angiopoietin 1 and 2 Neutralizing Peptibody, Combined with Pembrolizumab in Patients with Advanced Ovarian and Colorectal Cancer. (PubMed, Cancer Immunol Res)
After development of acquired resistance, biopsy of one patient's KRAS wild-type, ERBB2 amplified tumor showed a substantial decline in tumor-associated T cells and an increase in immunosuppressive intratumoral macrophages. Future studies are needed to carefully assess whether clinicogenomic features, such as lack of liver metastases, ERBB2 amplification, and left-sided tumors, can predict increased sensitivity to PD1 immunotherapy combinations.
P1 data • Journal • PD(L)-1 Biomarker • IO biomarker • Metastases
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HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • POLE (DNA Polymerase Epsilon)
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HER-2 amplification • POLE mutation • KRAS wild-type • RAS wild-type
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Keytruda (pembrolizumab) • trebananib (AMG 386)
2ms
ESM1 facilitates the EGFR/HER3-triggered epithelial-to-mesenchymal transition and progression of gastric cancer via modulating interplay between Akt and angiopoietin-2 signaling. (PubMed, Int J Biol Sci)
Furthermore, therapeutic peptides successfully inhibited ESM1's induction of the aforementioned signals and motility of GC cells. ESM1's oncogenic role in GC involves activating the EGFR/HER3-Akt/ANGPT2 pathway, presenting a potential therapeutic target for GC.
Journal
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EGFR (Epidermal growth factor receptor) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • ESM1 (Endothelial Cell Specific Molecule 1)
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EGFR exon 19 deletion
2ms
SPRi Biosensor for Simultaneous Determination of HIF-1α, Angiopoietin-2, and Interleukin-1β in Blood Plasma. (PubMed, Sensors (Basel))
However, the constructed biosensor is characterized by its ease and speed of measurement, and the method does not require special preparation of samples. SPRi biosensors can be used as a sensitive and highly selective method for determining potential blood biomarkers, which in the future may become part of the routine diagnosis of cancers.
Journal
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HIF1A (Hypoxia inducible factor 1, alpha subunit) • IL1B (Interleukin 1, beta)
3ms
Evaluation of Therapeutic Efficacy of Faricimab for Clinical AMD, DME, and RVO Patients (clinicaltrials.gov)
P2/3, N=30, Recruiting, Second Affiliated Hospital, School of Medicine, Zhejiang University
New P2/3 trial
3ms
Intravitreal Faricimab Injections or Fluocinolone Acetonide (0.19 mg) Intravitreal Implants vs Observation for Prevention of VA Loss Due to Radiation Retinopathy (clinicaltrials.gov)
P3, N=600, Recruiting, Jaeb Center for Health Research | Trial completion date: Nov 2028 --> Dec 2029 | Trial primary completion date: Nov 2026 --> Dec 2029
Trial completion date • Trial primary completion date
4ms
Pre-operative Vabysmo in Patients With Non-clearing Vitreous Hemorrhage Secondary to Proliferative Diabetic Retinopathy (clinicaltrials.gov)
P4, N=100, Enrolling by invitation, University of Colorado, Denver | Not yet recruiting --> Enrolling by invitation
Enrollment open
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Avastin (bevacizumab)
4ms
Trial primary completion date • Combination therapy • Metastases
|
SIRPA (Signal Regulatory Protein Alpha)
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Erbitux (cetuximab) • paclitaxel • docetaxel • capecitabine • ezabenlimab (BI 754091) • BI 765063 • BI 836880
5ms
Trial primary completion date
6ms
Analysis of Changes of Ang-2 and TNF-α Levels in Patients with AMI Complicated with Pulmonary Infection and Drug Resistance of Infectious Pathogens. (PubMed, Altern Ther Health Med)
Increased levels of angiopoietin-2 and tumor necrosis factor α were observed. Early detection of these markers can assist in the clinical diagnosis and guide the appropriate use of antibiotics.
Journal
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TNFA (Tumor Necrosis Factor-Alpha) • MB (Myoglobin)
6ms
Pre-operative Vabysmo in Patients With Non-clearing Vitreous Hemorrhage Secondary to Proliferative Diabetic Retinopathy (clinicaltrials.gov)
P4, N=100, Not yet recruiting, University of Colorado, Denver | Initiation date: Mar 2024 --> Aug 2024
Trial initiation date
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Avastin (bevacizumab)
6ms
NRASQ61R mutation drives elevated angiopoietin-2 expression in human endothelial cells and a genetic mouse model. (PubMed, Pediatr Blood Cancer)
Our studies show that the NRASQ61R mutation in endothelial cells induces Ang-2 expression in vitro and in vivo. In cultured human endothelial cells, NRASQ61R drives elevated Ang-2 through MAP kinase and mTOR-dependent signaling pathways.
Preclinical • Journal
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ANGPT2 (Angiopoietin 2)
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NRAS mutation • NRAS Q61 • NRAS wild-type • NRAS Q61R • ANG elevation • ANGPT2 expression
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Mekinist (trametinib) • sirolimus
7ms
Angiopoietin-2, vascular endothelial growth factor family, and heparin binding endothelial growth factor are associated with subclinical atherosclerosis in rheumatoid arthritis. (PubMed, Comput Struct Biotechnol J)
In women, angiopoietin-2 was associated with PWV (β = 0.18). The selected GFs were closely related to atherosclerosis in patients with RA and are potential predictors of CV disease in patients with RA.
Journal
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VEGFA (Vascular endothelial growth factor A) • VEGFD (Vascular Endothelial Growth Factor D) • VEGFC (Vascular Endothelial Growth Factor C)
7ms
A Study to Test Whether Different Combinations of BI 765063, Ezabenlimab, Chemotherapy, Cetuximab, and BI 836880 Help People With Head and Neck Cancer or Liver Cancer (clinicaltrials.gov)
P1, N=48, Active, not recruiting, Boehringer Ingelheim | Recruiting --> Active, not recruiting | Trial primary completion date: Apr 2025 --> Nov 2024
Enrollment closed • Trial primary completion date • Combination therapy • Metastases
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SIRPA (Signal Regulatory Protein Alpha)
|
Erbitux (cetuximab) • paclitaxel • docetaxel • capecitabine • ezabenlimab (BI 754091) • BI 765063 • BI 836880
7ms
MAGIC: Safety and Efficacy of Faricimab in Patients With NPDR (clinicaltrials.gov)
P2, N=150, Active, not recruiting, Greater Houston Retina Research | Recruiting --> Active, not recruiting
Enrollment closed
7ms
A Study to Test Whether Different Combinations of BI 765063, Ezabenlimab, Chemotherapy, Cetuximab, and BI 836880 Help People With Head and Neck Cancer or Liver Cancer (clinicaltrials.gov)
P1, N=45, Recruiting, Boehringer Ingelheim | Active, not recruiting --> Recruiting | Trial primary completion date: Aug 2024 --> Apr 2025
Enrollment open • Trial primary completion date • Combination therapy • Metastases
|
SIRPA (Signal Regulatory Protein Alpha)
|
Erbitux (cetuximab) • Tecentriq (atezolizumab) • paclitaxel • docetaxel • capecitabine • ezabenlimab (BI 754091) • BI 765063 • BI 836880
8ms
Enrollment closed • Combination therapy • Metastases
|
SIRPA (Signal Regulatory Protein Alpha)
|
Erbitux (cetuximab) • Tecentriq (atezolizumab) • paclitaxel • docetaxel • capecitabine • ezabenlimab (BI 754091) • BI 765063 • BI 836880
8ms
Pembrolizumab (Anti-PD-1) and AMG386 (Angiopoietin-2 (Ang-2) in Patients With Advanced Solid Tumor (clinicaltrials.gov)
P1, N=60, Active, not recruiting, Dana-Farber Cancer Institute | Trial completion date: Aug 2024 --> Aug 2025 | Trial primary completion date: Feb 2024 --> Feb 2025
Trial completion date • Trial primary completion date • Metastases
|
BRAF (B-raf proto-oncogene)
|
BRAF V600E • BRAF V600 • BRAF V600K
|
Keytruda (pembrolizumab) • trebananib (AMG 386)
9ms
Enrollment open
|
Lucentis (ranibizumab)
9ms
New trial
|
Lucentis (ranibizumab)
9ms
New trial
|
Eylea (aflibercept intravitreal) • Lucentis (ranibizumab)
9ms
AO: Home OCT-Guided Treatment Versus Treat and Extend for the Management of Neovascular AMD (clinicaltrials.gov)
P3, N=600, Recruiting, Jaeb Center for Health Research | Not yet recruiting --> Recruiting
Enrollment open
10ms
CCL18, CHI3L1, ANG2, IL-6 systemic levels are associated with the extent of lung damage and radiomic features in SARS-CoV-2 infection. (PubMed, Inflamm Res)
Data suggest a causal link between cytokines (risk factor), lung damage (mediator), and COVID-19 outcomes.
Journal
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IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • IL10 (Interleukin 10) • CHI3L1 (Chitinase 3-like 1) • LGALS3 (Galectin 3) • IL6R (Interleukin 6 receptor) • CCL18 (C-C Motif Chemokine Ligand 18)
10ms
Angiopoietin-2 and the Vascular Endothelial Growth Factor Promote Migration and Invasion in Hepatocellular Carcinoma- and Intrahepatic Cholangiocarcinoma-Derived Spheroids. (PubMed, Biomedicines)
Inhibitors targeting ANG-2 (Trebananib) and the VEGF (Bevacizumab) effectively blocked the migration ability of spheroids that had been stimulated with rh-ANG-2 and rh-VEGF. Overall, our findings highlight the critical role played by ANG-2 and the VEGF in enhancing the ability of HCC- and iCCA-derived spheroids to migrate and invade, which are key processes in cancer progression.
Journal
|
VEGFA (Vascular endothelial growth factor A) • CDH1 (Cadherin 1) • VIM (Vimentin) • CDH2 (Cadherin 2)
|
Avastin (bevacizumab) • trebananib (AMG 386)
10ms
FAN: Faricimab for High-frequent Aflibercept Treated Neovascular Age-related Macular Degeneration (clinicaltrials.gov)
P4, N=70, Active, not recruiting, Medical University of Graz | Recruiting --> Active, not recruiting | Trial primary completion date: Jun 2024 --> Oct 2024
Enrollment closed • Trial primary completion date
|
VEGFA (Vascular endothelial growth factor A)
|
Eylea (aflibercept intravitreal)
10ms
Journal
|
CXCL10 (Chemokine (C-X-C motif) ligand 10)
11ms
New P4 trial
|
Avastin (bevacizumab)
11ms
Enrollment open
11ms
Neoadjuvant trebananib plus paclitaxel-based chemotherapy for stage II/III breast cancer in the adaptively randomized I-SPY2 trial - Efficacy and biomarker discovery. (PubMed, Clin Cancer Res)
The Ang/Tie2 axis inhibitor trebananib combined with standard neoadjuvant therapy increased estimated pCR rates across HR-negative and MP2 subtypes, with probabilities of superiority >90%. Further study of Ang/Tie2 receptor axis inhibitors in validated, biomarker-predicted sensitive subtypes is warranted.
Journal
|
HER-2 (Human epidermal growth factor receptor 2) • CD8 (cluster of differentiation 8)
|
HER-2 positive • HER-2 negative • HER-2 expression • CD8 expression
|
MammaPrint
|
Herceptin (trastuzumab) • paclitaxel • doxorubicin hydrochloride • cyclophosphamide • trebananib (AMG 386)
11ms
Single Injection of Faricimab for nAMD With Persisting Fluid Despite Frequent Aflibercept Treatments (clinicaltrials.gov)
P=N/A, N=46, Completed, Rigshospitalet, Denmark | Active, not recruiting --> Completed
Trial completion
|
Eylea (aflibercept intravitreal)
12ms
Enrollment change
|
Erbitux (cetuximab) • Tecentriq (atezolizumab) • paclitaxel • docetaxel • capecitabine • ezabenlimab (BI 754091) • BI 765063 • BI 836880
1year
Trial completion
|
BI 836880
1year
New trial
|
Eylea (aflibercept intravitreal)
1year
5α-Hydroxycostic acid inhibits choroidal neovascularization in rats through a dual signalling pathway mediated by VEGF and angiopoietin 2. (PubMed, Mol Med)
5α-Hydroxycostic acid can inhibit choroidal neovascularization by interfering with the VEGF- and Ang2/Tie2-related pathways, and it may be a good candidate drug for treating CNV.
Preclinical • Journal
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KDR (Kinase insert domain receptor)