Zika virus has been an important cause of neurovirulence in humans. It is a global health concern due to its association with the Guillain-Barré syndrome in adults and congenital birth defects in neonates. Despite its re-emergence in the outbreaks of 2015-16, there is no approved drug for the treatment of Zika virus infection till date making it a subject of immediate attention and intervention. Both recent and earlier efforts in drug repurposing and viral vaccine development seem to offer a favourable roadmap to mitigate Zika virus infections. Promising molecules under investigation commonly target viral proteins, protein precursors, and complexes, and interfere with host pathways involving cellular kinases, glucose transporter and NMDA receptors. Repositioned drug candidates like niclosamide, favipiravir, and chloroquine exhibit promising antiviral potential. In parallel, anti-ZIKV vaccines like VRC-ZKADNA090-00-VP, AGS-v, and mRNA-1325 have progressed to early-phases of clinical trials achieving acceptable safety and immunogenic profiles. CRISPR-Cas13b based genome editing have also been successfully demonstrated to cleave Zika virus ssRNA in infected cells. Present review elucidates the pathogenesis of Zika virus infection, and provides an in-depth overview of the current strategies and research aimed at targeting host and viral factors to avail successful therapeutic outcomes. Review also underscores the importance of safety evaluation of the developmental drugs in pregnancy owing to the strong association of ZIKV and fetal birth defects.