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  • ||||||||||  AiTan (rivoceranib) / HLB Bio Group
    Enrollment open, Trial completion date, Trial initiation date, Trial primary completion date:  TMZ Plus Apatinib in Newly Diagnosed High-grade Glioma?RCT (clinicaltrials.gov) -  Jul 22, 2019   
    P2,  N=211, Recruiting, 
    Apatinib plus docetaxel, as the second or above line treatment, is effective and safe against advanced nonsquamous NSCLC, with good tolerance profile. Not yet recruiting --> Recruiting | Trial completion date: Jul 2022 --> Feb 2023 | Initiation date: Feb 2019 --> May 2019 | Trial primary completion date: Feb 2022 --> Oct 2022
  • ||||||||||  AiTan (rivoceranib) / HLB Bio Group
    Trial completion date, Trial initiation date, Trial primary completion date:  Combination Neoadjuvant Chemotherapy With or Without Apatinib for HER2 Negative Breast Cancer (clinicaltrials.gov) -  Jul 17, 2019   
    P2,  N=196, Recruiting, 
    Trial registration This study was registered on ClinicalTrials.gov (NCT01762293) and was orally presented in the 2015 ASCO-Gastrointestinal Symposium. Trial completion date: Oct 2022 --> Apr 2023 | Initiation date: Oct 2018 --> Apr 2019 | Trial primary completion date: Apr 2022 --> Oct 2022
  • ||||||||||  Cabometyx (cabozantinib tablet) / Takeda, Exelixis, Ipsen
    Journal:  Emerging multitarget tyrosine kinase inhibitors in the treatment of neuroendocrine neoplasms. (Pubmed Central) -  Jul 17, 2019   
    ...The multitarget tyrosine kinase inhibitor (MTKI), sunitinib malate, has been approved by Regulatory Agencies in pancreatic NENs...An in-depth review on the studies published on the MTKIs in neuroendocrine tumors such as axitinib, cabozantinib, famitinib, lenvatinib, nintedanib, pazopanib, sorafenib and sulfatinib was performed...Moreover, for the first time in the literature, we report an updated view concerning the upcoming clinical trials in this field: presently, phase I, II, and III clinical trials are ongoing and will include, overall, a staggering 1667 patients. This fervid activity underlines the increasing interest of the scientific community in the use of emerging MTKIs in NEN treatment.
  • ||||||||||  camrelizumab (INCSHR1210) / Incyte
    Journal:  Anti-PD1 'SHR-1210' aberrantly targets pro-angiogenic receptors and this polyspecificity can be ablated by paratope refinement. (Pubmed Central) -  Jul 17, 2019   
    The combination of receptor proteome screening and optimization of the antibody binding interface therefore succeeded in generating novel, higher-potency, specificity-enhanced therapeutic IgGs from a single, clinically sub-optimal progenitor. This study showed that highly-specific off-target binding events might be an under-appreciated phenomenon in therapeutic antibody development, but that these unwanted properties can be fully ameliorated by paratope refinement.
  • ||||||||||  AiTan (rivoceranib) / Elevar Therapeutics
    Trial completion, Phase classification, Trial completion date, Trial primary completion date:  A Study of Second-line Treatment With Apatinib in Patients With Advanced Intrahepatic Cholangiocarcinoma (clinicaltrials.gov) -  Jul 15, 2019   
    P2,  N=34, Completed, 
    This study showed that highly-specific off-target binding events might be an under-appreciated phenomenon in therapeutic antibody development, but that these unwanted properties can be fully ameliorated by paratope refinement. Recruiting --> Completed | Phase classification: P3 --> P2 | Trial completion date: Sep 2018 --> May 2019 | Trial primary completion date: Aug 2018 --> Mar 2019
  • ||||||||||  AiTan (rivoceranib) / LSK BioPartners
    Preclinical, Journal:  Apatinib exhibits anti-leukemia activity in preclinical models of acute lymphoblastic leukemia. (Pubmed Central) -  Jul 11, 2019   
    Recruiting --> Completed | Phase classification: P3 --> P2 | Trial completion date: Sep 2018 --> May 2019 | Trial primary completion date: Aug 2018 --> Mar 2019 Our study indicates that Apatinib exerts its anti-leukemia effect by inducing apoptosis through suppressing the VEGFR2 signaling pathway, supporting a potential role for Apatinib in the treatment of ALL.
  • ||||||||||  AiTan (rivoceranib) / LSK BioPartners
    Retrospective data, Journal:  A retrospective study of low-dose apatinib combined with S-1 in patients with advanced non-small cell lung cancer. (Pubmed Central) -  Jul 10, 2019   
    Treatment-related grade III toxicity was observed in 5 patients (16%) and common grade I or II adverse events (AEs) were fatigue (42%), hypertension (32%), and hand-foot-skin reaction (23%). Combination of low-dose apatinib and S-1 could be an effective and tolerable choice for advanced NSCLC patients who are unable to benefit from standard treatment; however, further exploration in larger clinical trials is needed.
  • ||||||||||  AiTan (rivoceranib) / HLB Bio Group
    Trial primary completion date, Monotherapy, Metastases:  Apatinib for the Elderly Advanced Gastric Cancer (clinicaltrials.gov) -  Jul 8, 2019   
    P2,  N=60, Recruiting, 
    Combination of low-dose apatinib and S-1 could be an effective and tolerable choice for advanced NSCLC patients who are unable to benefit from standard treatment; however, further exploration in larger clinical trials is needed. Trial primary completion date: Jun 2019 --> Dec 2019
  • ||||||||||  AiRuiLi (adebrelimab) / Jiangsu Hengrui Pharma
    Trial completion date, PD(L)-1 Biomarker, IO biomarker:  A Trial to Evaluate Safety and Tolerability of SHR-1316 in Cancer Patients (clinicaltrials.gov) -  Jul 5, 2019   
    P1,  N=37, Active, not recruiting, 
    Trial primary completion date: Jun 2019 --> Dec 2019 Trial completion date: May 2019 --> Sep 2019
  • ||||||||||  Zaltrap (ziv-aflibercept IV) / Sanofi, Regeneron, Avastin (bevacizumab) / Roche
    Biomarker, Clinical, Review, Journal:  Safety and Tolerability of Anti-Angiogenic Protein Kinase Inhibitors and Vascular-Disrupting Agents in Cancer: Focus on Gastrointestinal Malignancies. (Pubmed Central) -  Jun 30, 2019   
    Second-line ramucirumab and third-line apatinib are effective anti-angiogenic treatments for patients with metastatic gastric cancer...Anti-angiogenic agents may be more effective in combination therapies, with not only cytotoxics but also other emerging compounds in the anti-angiogenic class or in the separate class of the so-called vascular-disrupting agents. This review aims to provide an overview of the approved and "under development" anti-angiogenic compounds as well as the vascular-disrupting agents in the treatment of gastrointestinal cancers, focusing on the actual body of knowledge available on therapy challenges, pharmacodynamic and pharmacokinetic mechanisms, safety profiles, promising predictive biomarkers, and future perspectives.
  • ||||||||||  AiSuDa (ivarmacitinib) / Jiangsu Hengrui Pharma, Arcutis
    Trial initiation date, Trial primary completion date:  AMBER2: A Phase II Study in Patients With Moderate to Severe Active Ulcerative Colitis. (clinicaltrials.gov) -  Jun 27, 2019   
    P2,  N=152, Recruiting, 
    Apatinib therapy beyond progression could provide further benefits in specific subpopulations. Initiation date: Dec 2018 --> Apr 2019 | Trial primary completion date: Apr 2020 --> Jul 2020
  • ||||||||||  AiTan (rivoceranib) / LSK BioPartners
    Clinical, Observational data, Journal, Combination therapy:  Safety and efficacy of combination therapy with apatinib and doxorubicin in metastatic soft tissue sarcomas: an observational study from multiple institutions. (Pubmed Central) -  Jun 27, 2019   
    Grade 3-4 adverse events were more common with apatinib plus doxorubicin than with apatinib after doxorubicin, and these included leukopenia (5.45% vs 38.1%, respectively, p=0.001), anemia (7.27% vs 28.57%, respectively, p=0.023), oral mucositis (3.64% vs 19.05%, respectively, p=0.046), transaminase increases (0% vs 14.29%, respectively, p=0.011). Our results do not support the use of apatinib plus doxorubicin for metastatic STS unless the specific objective is tumor shrinkage.
  • ||||||||||  AiTan (rivoceranib) / HLB Bio Group
    Trial completion:  Apatinib Combined With Oral Etoposide in Metastatic HER2 Negative Breast Cancer (clinicaltrials.gov) -  Jun 25, 2019   
    P2,  N=32, Completed, 
    The combination treatment of MBRI-001 and sorafenib exhibited a higher antitumor effect, which could provide a new strategy to treat HCC in the future. Recruiting --> Completed
  • ||||||||||  camrelizumab (INCSHR1210) / Incyte
    Journal:  Discovery of Imidazoisoindole Derivatives as Highly Potent and Orally Active Indoleamine-2,3-dioxygenase Inhibitors. (Pubmed Central) -  Jun 23, 2019   
    Lead optimization toward improving potency and eliminating CYP inhibition resulted in the discovery of lead compound 25, a highly potent IDO inhibitor with favorable pharmacokinetic properties. In the MC38 xenograft model in hPD-1 transgenic mice, 25 in combination with the anti-PD-1 monoclonal antibody (SHR-1210) achieved a synergistic antitumor effect superior to each single agent.
  • ||||||||||  AiTan (rivoceranib) / LSK BioPartners
    Journal:  Apatinib enhances chemosensitivity of gastric cancer to paclitaxel and 5-fluorouracil. (Pubmed Central) -  Jun 21, 2019   
    The experimental data suggested that apatinib improves the efficacy of PTX and 5-Fu both in vitro and in vivo. Clinical evidence showed that a combination of PS chemotherapy with apatinib may be an efficient and acceptable safety treatment for late-stage GC, especially in conversion surgery.
  • ||||||||||  AiTan (rivoceranib) / HLB Bio Group
    Apatinib inhibits glycolysis by suppressing VEGFR2/AKT1/SOX5/GLUT4 signaling pathway in ovarian cancer (Exhibition and Poster Viewing Area) -  Jun 19, 2019 - Abstract #IGCS2019IGCS_836;    
    Randomised controlled trials are needed to further establish the role of immune checkpoint inhibition for nasopharyngeal carcinomas. We provide new evidence that apatinib suppresses cell proliferation and glycolysis by inhibiting VEGFR2/AKT1/GSK3β/SOX5/GLUT4 signaling pathway in ovarian cancer cells, suggesting that apatinib may be a very promising drug for the treatment of ovarian cancer.
  • ||||||||||  AiTan (rivoceranib) / LSK BioPartners, Spherazole (itraconazole) / RA Chem, JW Pharma, Spherics, Vocozo (voriconazole) / Orchid
    PK/PD data, Preclinical, Journal:  Effects of ketoconazole, voriconazole, and itraconazole on the pharmacokinetics of apatinib in rats. (Pubmed Central) -  Jun 17, 2019   
    Apatinib can be co-administered with itraconazole, but ketoconazole and voriconazole should be avoided if possible or be underwent therapeutic drug monitoring of apatinib. A further clinical study should be conducted to investigate the inhibitory effect of azole antifungal drugs on the apatinib plasma concentration.
  • ||||||||||  AiTan (rivoceranib) / Elevar Therapeutics
    Enrollment closed:  A Study of Fluzoparib Given in Combination With Apatinib in Ovarian or Breast Cancer Patients (clinicaltrials.gov) -  Jun 17, 2019   
    P1,  N=98, Active, not recruiting, 
    A further clinical study should be conducted to investigate the inhibitory effect of azole antifungal drugs on the apatinib plasma concentration. Recruiting --> Active, not recruiting
  • ||||||||||  AiRuiYi (fluzoparib) / Jiangsu Hengrui Pharma
    Trial completion, Enrollment change:  A Phase I Study of Fluzoparib in Patient With Advanced Solid Malignancies (clinicaltrials.gov) -  Jun 17, 2019   
    P1,  N=79, Completed, 
    Recruiting --> Active, not recruiting Recruiting --> Completed | N=42 --> 79
  • ||||||||||  AiTan (rivoceranib) / LSK BioPartners
    Journal, IO Biomarker:  Apatinib regulates the cell proliferation and apoptosis of liver cancer by regulation of VEGFR2/STAT3 signaling. (Pubmed Central) -  Jun 15, 2019   
    Compared with control group, Apatinib significantly induced BAX/Bcl-2 ratio elevation, reduced p-STAT3 and p-VEGFR2 expression, which were significantly augmented by the treatment of siSTAT3. In conclusion, Apatinib inhibited the cell proliferation and promoted the cell apoptosis of liver cancer by inhibiting the activation of VEGFR2/STAT3.