Visceral leishmaniasis (VL) or Kala-azar, is the most lethal form of leishmaniasis, is still prevalent in many countries where it is endemic. It is a threat to human life caused by protozoan parasite Leishmania donovani. The severity of the disease is further increased as the treated individuals might have a chance of developing Post Kala-azar Dermal Leishmaniasis (PKDL) in the long run. Moreover, several countries have reported high number of HIV-VL co-infected patients. Therefore, there is a dire need for the development of efficient diagnostic methods and drugs in order to combat the disease and to control the spread of disease. At present, the treatment for VL entirely relies on therapeutic drugs as no vaccine is available yet. Ever since 1900s a series of drugs have been invented and used for treatment of VL; but the need for one such cost-effective treatment that would completely cure the disease with minimal side-effects, low relapse rate with high efficacy and less toxicity remains yet to be fulfilled. Therefore, identifying novel compounds is very crucial to develop potent antileishmanial agents. Thus, this review enlists several instances of drug development, including the pharmacokinetic and pharmacodynamic properties of antileishmanial drugs, different experimental animal models used to investigate the disease progression and to analyze treatment dosage and pharmacological aspect of drugs. Furthermore, the existing gap in drug development and future measures to improve the process are also discussed in this review.