Phase II study of an AKT inhibitor MK2206 in patients with relapsed or refractory lymphoma

Br J Haematol. 2015 Nov;171(4):463-70. doi: 10.1111/bjh.13603. Epub 2015 Jul 27.

Abstract

We conducted a phase II study of the AKT inhibitor, MK2206 in patients with relapsed or refractory lymphoma of any histology excluding Burkitt lymphoma or lymphoblastic lymphoma. MK-2206 was administered orally at 200 mg once weekly in 28-d cycles up to 12 cycles in the absence of progression or significant toxicity. The dose was adjusted based on tolerance. A total of 59 patients were enrolled. The final doses patients received were 300 mg (n = 33), 250 mg (n = 2), 200 mg (n = 16) and 135 mg (n = 8). Based on intent-to-treat analysis, objective response was observed in 8 (14%) patients (2 complete response and 6 partial response), with median response duration of 5·8 months. The overall response rate was 20% in 25 patients with classical Hodgkin lymphoma. Rash was the most common toxicity (any grade 53%, Grade 3 in 15%) and was observed in a dose-dependent manner. The correlative cytokine analysis showed paradoxical increase in several cytokines, which may be explained by negative feedback mechanism induced by the on-target effect of AKT inhibitor. Our data demonstrate that MK2206 has a favourable safety profile with a modest activity in patients with relapsed Hodgkin lymphoma. The future studies should explore mechanism-based combinations (clinicaltrials.gov NCT01258998).

Keywords: AKT; clinical trials; lymphoma; target therapy.

Publication types

  • Clinical Trial, Phase II
  • Research Support, N.I.H., Extramural

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Antineoplastic Agents / adverse effects
  • Antineoplastic Agents / therapeutic use*
  • Combined Modality Therapy
  • Cytokines / blood
  • Disease-Free Survival
  • Dose-Response Relationship, Drug
  • Drug Eruptions / etiology
  • Feedback, Physiological
  • Female
  • Gastrointestinal Diseases / chemically induced
  • Hematologic Diseases / chemically induced
  • Hematopoietic Stem Cell Transplantation
  • Heterocyclic Compounds, 3-Ring / adverse effects
  • Heterocyclic Compounds, 3-Ring / therapeutic use*
  • Hodgkin Disease / blood
  • Hodgkin Disease / drug therapy
  • Hodgkin Disease / enzymology
  • Humans
  • Hyperglycemia / chemically induced
  • Kaplan-Meier Estimate
  • Lymphoma / blood
  • Lymphoma / drug therapy*
  • Lymphoma / enzymology
  • Lymphoma / therapy
  • Male
  • Middle Aged
  • Neoplasm Proteins / antagonists & inhibitors*
  • Protein Kinase Inhibitors / adverse effects
  • Protein Kinase Inhibitors / therapeutic use*
  • Proto-Oncogene Proteins c-akt / antagonists & inhibitors*
  • Recurrence
  • Salvage Therapy
  • Transplantation, Autologous
  • Treatment Outcome
  • Tumor Burden / drug effects
  • Young Adult

Substances

  • Antineoplastic Agents
  • Cytokines
  • Heterocyclic Compounds, 3-Ring
  • MK 2206
  • Neoplasm Proteins
  • Protein Kinase Inhibitors
  • AKT1 protein, human
  • Proto-Oncogene Proteins c-akt

Associated data

  • ClinicalTrials.gov/NCT01258998