Mushrooms represent a large family of fleshy fungi that have been of high interest since ancient ages due to their medicinal and nutritional importance. Therefore, it can represent a significant source of bioactive compounds in malaria control. The few numbers of studies on <i>in vitro</i> antiplasmodial and insecticidal properties of their extracts and chemical constituents led to interesting results reported in numerous scientific publications. This review aims to provide a comprehensive compilation of literature up to 2021 on the antiplasmodial, insecticidal as well as cytotoxic chemical constituents of medicinal mushrooms that can help in the management of malaria both against the parasite <i>Plasmodium falciparum</i> and the mosquitoe <i>Anopheles stephensis</i> acting as a vector of malaria through its bites. For this purpose, some searches have been done in some online libraries using keywords like Basidiomycete, mushroom, malaria, <i>Plasmodium</i>, <i>Anopheles</i> and antiplasmodial without language restriction. Among the reported compounds, 51 selected ones displayed significant antiplasmodial potency with IC<sub>50</sub> values lower than 10 μM against <i>P. falciparum</i> strains sensitive or resistant to chloroquine. For instance, ganoderic acid AW1 demonstrated a strong antiplasmodial activity with IC<sub>50</sub> of 257.8 nM against <i>P. falciparum</i> D6, while strong activities were displayed by ganoweberianones A (IC<sub>50</sub> = 0.050 μM) and B (IC<sub>50</sub> = 0.46 μM) against <i>P. falciparum</i> K1. Moreover, some mushroom methanol extracts demonstrated good larvicidal and ovicidal activities against <i>Anopheles stephensis</i>. This paper provides further insights into the development of new antiplasmodial drugs or new potent eco-friendly pesticides to control mosquito vectors.