Use of Oral Dichloroacetate for Palliation of Leg Pain Arising from Metastatic Poorly Differentiated Carcinoma: A Case Report

Abstract

Dichloroacetate sodium (DCA) is a nonproprietary drug currently used for treatment of inherited mitochondrial diseases. It was discovered in 2007 that DCA promotes human cancer cell death by a novel mechanism. Soon after this discovery, physicians began using DCA off-label for cancer treatment in a palliative setting. A case report is presented of a 71-year-old male with poorly differentiated carcinoma of unknown primary metastatic to the right leg and liver who achieved excellent palliation of leg pain by using oral DCA after failing conventional therapy.

Anticancer Agents That Counteract Tumor Glycolysis

“…[238, 313] Palliative use of DCA in the presence of a metastatic carcinoma caused a beneficial pain reduction, as well as a certain stabilization of the growth of metastases. [314] As for side effects, DCA seems to be a relatively safe anticancer agent, causing only a certain dose-dependent reversible peripheral nerve toxicity. [315] At the molecular level, DCA binds at the pyruvate binding site in the N -terminal regulatory (R) domain of PDK, establishing strong attractive interaction with arginine residues (Arg154 in PDK2), with various levels of potencies on each enzyme subtype ranging around the millimolar concentration (PDK1: K i =1 mM; PDK2: K i =0.2 mM; PDK3: K i =8 mM; PDK4, K i =0.5 mM).…”

The Biological Activity of Sodium Dichloroacetate and Its Effectiveness During the Experimental Clinical Studies

“…Описывается клинический случай, в котором 71-летний пациент с низкодифференцированным метастатическим раком принимал НДХА в каче-стве паллиативного лечения [22]. Спустя 5 меся-цев после начала терапии качество жизни боль-ного заметно улучшилось за счет купирования болевого синдрома в ноге, в результате чего был прекращен прием всех обезболивающих препа-ратов [22].…”

“…Спустя 5 меся-цев после начала терапии качество жизни боль-ного заметно улучшилось за счет купирования болевого синдрома в ноге, в результате чего был прекращен прием всех обезболивающих препа-ратов [22]. В другом исследовании описывается наблюдение за 18 пациентами с опухолями пан-креатических и желчных протоков, принимавшими НДХА в комбинации с омепразолом.…”

The Pyruvate Dehydrogenase Complex in Cancer: Implications for the Transformed State and Cancer Chemotherapy

“…DCA is a cheap, generic drug and no corporate actors have an incentive to develop the agent. To date clinical data consist of several anecdotal case reports [66,67] suggesting possible efficacy, including in a poorly differentiated metastatic carcinoma. In addition, in view of its low cost and wide availability, DCA is being prescribed off-label or self-administered.…”