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Background and Objectives: Autism spectrum disorder (ASD) is a heterogeneous neuro-developmental condition characterized by social communication deficits, restricted interests, and repetitive behaviors. Pharmacological management is challenging given the complex neurobiology and frequent comorbidities. This review summarizes the current evidence for pharmacological treatments in ASD, highlighting efficacy, mechanisms, limitations, and emerging therapeutic targets. Methods: A comprehensive literature review was conducted across PubMed, Cochrane Library, and Embase to identify clinical trials, systematic reviews, meta-analyses, and preclinical studies on pharmacological interventions for ASD. Seventy-seven references were integrated to reflect the state of evidence. Results: Established interventions include antipsychotics such as risperidone and aripiprazole for irritability and aggression, and selective serotonin reuptake inhibitors (SSRIs) for anxiety and repetitive behaviors, though efficacy remains inconsistent. Adjunctive agents targeting glutamatergic, GABAergic, and neuroinflammatory pathways—including memantine, riluzole, minocycline, and N-acetylcysteine—show promise in modulating ex-citatory-inhibitory imbalance and oxidative stress. Novel strategies involving oxytocin, vasopressin, and nanoparticle-based therapies are under early investigation. Conclusions: While current pharmacologic options in ASD remain limited, advances in understanding neurotransmission, immune dysregulation, and neuroplasticity are driving innovation. Personalized approaches integrating biomarkers, genetics, and mechanistic targets may guide the next generation of therapies.