Due to the multifactorial nature of Alzheimer’s disease (AD), therapy using single protein/gene delivery has thus far failed resulting in the emergence of alternative therapeutic strategies comprising of multiple proteins/genes to treat multiple targets in AD. Another major obstacle current AD therapeutics face is the impaired penetration of neuroactive drugs through the blood brain-barrier (BBB). Similarly, photodynamic therapy although has revolutionized the medical science but the use of a permanently implanted fiber as an external light source (to activate the photosensitizer) has become the biggest drawback of photodynamic therapy of brain disorders like AD. Here, I propose to ferry a multitarget-directed therapeutic via receptor-mediated transcytosis across the BBB by fusing it with a BBB molecular Trojan horse that quickly switches into an aggressive photoactive molecule to destroy even the residual amyloid plaques for Alzheimer’s therapy.