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DRUG:

Fujovee (abivertinib)

i
Other names: AC-0010, AC 0010, AC0010MA, STI-5656, AC0010, AC-0010MA, AC 0010MA
Company:
Sorrento
Drug class:
EGFR inhibitor, BTK inhibitor
Related drugs:
3ms
Avitinib suppresses NLRP3 inflammasome activation and ameliorates septic shock in mice (PubMed, Nan Fang Yi Ke Da Xue Xue Bao)
Avitinib suppresses NLRP3 inflammasome activation and alleviates septic shock in mice.
Preclinical • Journal
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IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • IL1B (Interleukin 1, beta) • NLRP3 (NLR Family Pyrin Domain Containing 3) • CASP1 (Caspase 1)
|
Fujovee (abivertinib)
6ms
Drug-drug interactions between epidermal growth factor receptor tyrosine kinase inhibitors and rivaroxaban in vitro and in vivo. (PubMed, PLoS One)
These findings confirm the presence of DDIs between EGFR TKIs and rivaroxaban. Avitinib and gefitinib significantly inhibit rivaroxaban metabolism, and their co-administration may aggravate the risk of bleeding.
Preclinical • Journal
|
EGFR (Epidermal growth factor receptor) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
|
gefitinib • Fujovee (abivertinib)
over2years
Evaluating the efficacy and cardiotoxicity of EGFR-TKI AC0010 with a novel multifunctional biosensor. (PubMed, Microsyst Nanoeng)
This is the first study in which the risk of AC0010-induced cardiotoxicity was evaluated. In addition, novel multifunctional biosensors can comprehensively evaluate the antitumor efficacy and cardiotoxicity of drugs and candidate compounds.
Journal
|
EGFR mutation • EGFR L858R • EGFR T790M • EGFR wild-type • EGFR L858R + EGFR T790M • EGFR H1975
|
Fujovee (abivertinib)
over2years
Trial suspension • Combination therapy • Metastases
|
HSD3B1 (Hydroxy-Delta-5-Steroid Dehydrogenase 3 Beta- And Steroid Delta-Isomerase 1)
|
abiraterone acetate • Fujovee (abivertinib)
over2years
Antifibrotic mechanism of avitinib in bleomycin-induced pulmonary fibrosis in mice. (PubMed, BMC Pulm Med)
At present, only two drugs are approved by the FDA for the treatment of IPF, including the synthetic pyridinone drug, pirfenidone, and the tyrosine kinase inhibitor, nintedanib. The cellular experiments also indicated that avitinib improved alveolar epithelial cell injury in A549 cells. In conclusion, the present findings demonstrated that avitinib attenuates bleomycin-induced pulmonary fibrosis in mice by inhibiting alveolar epithelial cell injury and myofibroblast activation.
Preclinical • Journal
|
TGFB1 (Transforming Growth Factor Beta 1) • SMAD3 (SMAD Family Member 3)
|
nintedanib • bleomycin • Fujovee (abivertinib)
almost3years
Enrollment open • Combination therapy • Metastases
|
HSD3B1 (Hydroxy-Delta-5-Steroid Dehydrogenase 3 Beta- And Steroid Delta-Isomerase 1)
|
abiraterone acetate • Fujovee (abivertinib)
almost3years
Maverick: Study to Assess Abivertinib in Combination With Abiraterone in Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov)
P2, N=100, Not yet recruiting, Sorrento Therapeutics, Inc. | Initiation date: Oct 2022 --> Mar 2023
Trial initiation date • Combination therapy • Metastases
|
HSD3B1 (Hydroxy-Delta-5-Steroid Dehydrogenase 3 Beta- And Steroid Delta-Isomerase 1)
|
abiraterone acetate • Fujovee (abivertinib)
3years
Overview of the multifaceted resistances toward EGFR-TKIs and new chemotherapeutic strategies in non-small cell lung cancer. (PubMed, Biochem Pharmacol)
However, patients treated with third-generation TKIs (osimertinib, avitinib and rociletinib) targeting the EGFR T790M mutation have shown emerging resistances and relapses. This will pave the way for designing novel and effective chemotherapies to improve patients' overall survival. In this review, we provide an overview of the multifaceted mechanism of resistances towards EGFR-TKIs, as well as the challenges and perspectives that should be addressed in strategising chemotherapeutic treatments to overcome the ever evolving and adaptive nature of NSCLC.
Review • Journal
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR T790M
|
Tagrisso (osimertinib) • Xegafri (rociletinib) • Fujovee (abivertinib)
over3years
New P2 trial • Combination therapy
|
HSD3B1 (Hydroxy-Delta-5-Steroid Dehydrogenase 3 Beta- And Steroid Delta-Isomerase 1)
|
abiraterone acetate • Fujovee (abivertinib)
4years
Abivertinib inhibits megakaryocyte differentiation and platelet biogenesis. (PubMed, Front Med)
We also demonstrated in vivo that abivertinib decreased the number of MKs in bone marrow and platelet counts in mice, which suggested that thrombopoiesis was also inhibited. Thus, these preclinical data collectively suggested that abivertinib could inhibit MK differentiation and platelet biogenesis and might be an agent for thrombocythemia.
Journal
|
EGFR (Epidermal growth factor receptor) • BTK (Bruton Tyrosine Kinase) • CD34 (CD34 molecule) • JAK3 (Janus Kinase 3)
|
EGFR mutation
|
Fujovee (abivertinib)
4years
A novel third generation EGFR tyrosine kinase inhibitor Abivertinib for EGFR T790M mutant Non-Small Cell Lung Cancer: a multicenter phase1/2 study. (PubMed, Clin Cancer Res)
Abivertinib of 300 mg BID demonstrated favorable clinical efficacy with manageable side-effects in patients with EGFR T790M+NSCLC.
Clinical • P1/2 data • Journal
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR T790M
|
Fujovee (abivertinib)