Background: Malaria is a life-threatening disease prevalent in tropical and subtropical regions. Artemisinin combination therapy (ACT) used as an antimalarial treatment has reduced efficacy due to resistance, not only to the parasite but also to the vector. Therefore, it is important to find alternatives to overcome malaria cases through medicinal plants such as Ageratum conyzoides and other related plants within Asteraceae family. Purpose: This review summarizes the antimalarial and insecticidal activities of A. conyzoides and other plants belonging to Asteraceae family. Data Source: Google Scholar, PubMed, Science Direct, and Springer link. Study Selection: Online databases were used to retrieve journals using specific keywords combined with Boolean operators. The inclusion criteria were articles with experimental studies either in vivo or in vitro, in English or Indonesian, published after 1st January 2000, and full text available for inclusion in this review. Data Extraction: The antimalarial activity, insecticidal activity, and structure of the isolated compounds were retrieved from the selected studies. Data Synthesis: Antimalarial in vitro study showed that the dichloromethane extract was the most widely studied with an IC50 value <10 μg/mL. Among 84 isolated active compounds, 2-hydroxymethyl-non-3-ynoic acid 2-[2,2']-bithiophenyl-5-ethyl ester, a bithienyl compound from the Tagetes erecta plant show the smallest IC50 with value 0.01 and 0.02 µg/mL in Plasmodium falciparum MRC-pf-2 and MRC-pf-56, respectively. In vivo studies showed that the aqueous extract of A. conyzoides showed the best activity, with a 98.8% inhibition percentage using a 100 mg/kg dose of Plasmodium berghei (NK65 Strain). (Z)-γ-Bisabolene from Galinsoga parviflora showed very good insecticidal activity against Anopheles stephensi and Anopheles subpictus with LC50 values of 2.04 μg/mL and 4.05 μg/mL. Conclusion: A. conyzoides and other plants of Asteraceae family are promising reservoirs of natural compounds that exert antimalarial or insecticidal activity.