生物活性

• 描述Penfluridol has robust antipsychotic efficacy and is a first-generation diphenylbutylpiperidine. Its effects last for several days after a single oral dose and it can be administered once a week to provide better compliance and symptom control. In addition; the anti-cancer effects of penfluridol have been demonstrated in vivo: results showed slight changes in the volume and weight of organs at doses tested in animals^[3]. Penfluridol concentration-dependently suppressed the cell viability of AML cells with FLT3-WT (Fms-like tyrosine kinase 3) (HL-60 and U937) and FLT3-ITD (MV4-11); penfluridol's augmentation of intracellular ROS levels was critical for the penfluridol-induced autophagic response. The combination of penfluridol with an autophagy inhibitor may be a novel strategy for AML (acute myeloid leukemia) harboring FLT3-WT and FLT3-ITD^[4]. Penfluridol treatment suppressed the growth of BxPC-3 tumor xenografts by 48% as compared to 17% when treated in combination with chloroquine. Similarly, penfluridol suppressed the growth of AsPC-1 tumors by 40% versus 16% when given in combination with chloroquine^[5].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT03041233	-	-	Recruiting	March 27, 2020	Brazil ... more >> Cardioritmo Eletrofisiologia e Marpasso Recruiting Fortaleza, CE, Brazil Contact: Stela Sampaio, PhD    (85) 99984-6262    stelavsampaio@terra.com.br    Procardio Recruiting Fortaleza, CE, Brazil Contact: Evilásio da Silva, PhD    (85) 99219-4421    evilasioleobino@hotmail.com    Hospital Santa Rita Recruiting Vitória, ES, Brazil Contact: Fabricio Vassalo, PhD    (27) 99231-8545    fabricio@ceac-es.com.br    Vitoria Apart Hotel Recruiting Vitória, ES, Brazil Contact: Ricardo Kuniyoshi    (27) 99904-3057    r.r.k@uol.com.br    Eurolatino Recruiting Uberlândia, MP, Brazil Contact: Ruberval Rodrigues Santos, PhD    (34) 99964-4238    rubersantos1960@gmail.com    Cardioclin Recruiting João Pessoa, PB, Brazil Contact: André Queiroga, PhD    (83) 99106-7632    aaqueiroga@cardiol.br    Procardiaco Recruiting Rio de Janeiro, RJ, Brazil Contact: Eduardo Saad, PhD    (21) 98159-1000    eduardobsaad@hotmail.com    Unimed de Volta Redonda Recruiting Volta Redonda, RJ, Brazil Contact: Bruno Andrea, PhD    (21) 99992-6505    brunorandrea@gmail.com    Hospital São Vicente de Paulo Recruiting Passo Fundo, RS, Brazil Contact: José Basileu Reolão, PhD    (54) 99113-7213    basileu@terra.com.br    SOS Cardio Recruiting Florianopolis, SC, Brazil Contact: André D'Ávila, PhD    (48) 99929-9976    andredavila@mac.com    IPEMI - Instituto de Pesquisa e Estudos Médicos de Itajaí Recruiting Itajaí, SC, Brazil Contact: Tiago Silvestrini, PhD    (47) 99143-0713    tlsilvestrini@hotmail.com    Insitituto de Moléstias Cardiovasculares - IMC Recruiting São José do Rio Prêto, SP, Brazil Contact: Adalberto Filho, MD    (17) 3203-4051    dcimc@imconline.com.br    BP Recruiting São Paulo, SP, Brazil Contact: José Tarcício Vasconcelos    (11) 98507-2211    tarr@terra.com.br    SEMAP Recruiting São Paulo, SP, Brazil Contact: José Carlos Mateos, PhD    (11) 96397-0703    pachon@usp.br Collapse <<
  NCT03001141	-	-	Suspended(Waiting for ethical ... more >>re-evaluation) Collapse <<	February 2019	Brazil ... more >> Clinica Dom Rodrigo João Pessoa, PB, Brazil BP São Paulo, SP, Brazil, 01323-001 Instituto de Arritmias Cardíacas São Paulo, SP, Brazil, 01323-001 SEMAP São Paulo, SP, Brazil, 04.004-030 Collapse <<

• 参考文献

• [1] Flaim SF, Brannan MD, et al. Neuroleptic drugs attenuate calcium influx and tension development in rabbit thoracic aorta: effects of pimozide, penfluridol, chlorpromazine, and haloperidol. Proc Natl Acad Sci U S A. 1985 Feb;82(4):1237-41.

  [2] Creese I, Burt DR, Snyder SH. Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs. Science. 1976 Apr 30;192(4238):481-3.

  [3] Tuan NM, Lee CH. Penfluridol as a Candidate of Drug Repurposing for Anticancer Agent. Molecules. 2019;24(20):3659.

  [4] Wu SY, Wen YC, Ku CC, et al. Penfluridol triggers cytoprotective autophagy and cellular apoptosis through ROS induction and activation of the PP2A-modulated MAPK pathway in acute myeloid leukemia with different FLT3 statuses. J Biomed Sci. 2019;26(1):63.

  [5] Ranjan A, Srivastava SK. Penfluridol suppresses pancreatic tumor growth by autophagy-mediated apoptosis. Sci Rep. 2016;6:26165.

• 更多

• Collapse