THF (Tetrahydrofolate dehydrogenase)  Inhibitors Market: Competitive Landscape, Pipeline, and Market Analysis 2023

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Tetrahydrofolate dehydrogenase is an enzyme of the oxidoreductase family that catalysis the reaction yielding reduce folate or Tetrahydrofolate from Dihydrofolate in cells.  This Tetrahydrofolate is the substrate for purine ring synthesis, amino acid metabolism, and formation of deoxythymidine monophosphate. Tetrahydrofolate or Tetrahydro folic acid is the active form of folic acid. Folic acid is essential for the synthesis of RBCs and for maintaining brain health. THF dehydrogenase inhibitors block this pathway by acting on the enzyme THF dehydrogenase. These are used in treating many diseases like Rheumatoid Arthritis, Malaria, Traveller’s diarrhea, various types of cancers like breast cancer and non-Hodgkin’s lymphoma, and others in which the formation of folic acid or RBCs is involved. Businesses are looking for new and innovative chemicals to treat and prevent these diseases. Over the upcoming years, the market for THF dehydrogenase Inhibitors will witness significantly increased revenue due to the development and introduction of fresh products by industry participants. According to WHO, there were 247 million cases of malaria globally in 2021 as compared to 245 million patients in 2020. According to the Centers for Disease Control and Prevention (CDC), the highest malaria prevalence is in Africa. Developed nations have controlled the spread of malaria due to better health infrastructure and public health education but are at some risk of getting it back if held loose. Several of these inhibitors are on the market, while many are in ongoing clinical trials. 18 companies have various products in their pipelines, with 20 products in various stages of clinical trials. 1 product is in Phase 4, 6 products are in Phase 3, 7 products are in Phase 2, and 2 products are in Phase 1 of the clinical trials.

Key Developments of THF Dehydrogenase Inhibitors

  • In May 2019, Eisai entered into a licensing agreement with Medac GmbH to commercialize an Anti-rheumatic agent – Methotrexate sc injection in Japan.

Approved molecules

  • Metoject (methotrexate autopen)

Drugs in Pipeline

  • Folotyn (pralatrexate)
  • Pemfexy (pemetrexed)
  • Neutrexin (trimetrexate)
  • Otrexup (methotrexate)
  • iclaprim (MTF-100)
  • aminopterin
  • Xatmep (methotrexate oral solution)
  • LX-101
  • P218
  • methotrexate (ADX-2191)
  • methotrexate topical amphimatrix formulation (MQX-5902)
  • CH-1504
  • CH-4051
  • dapsone (PULM-001)

Clinical Activity and Developments of THF Dehydrogenase Inhibitors

  • As of June 2023, 18 companies have approximately 20 products for 471 diseases. For these diseases, more than 545 trials are being conducted by players globally. For instance,
  • Sanofi is conducting a Phase 3 clinical trial to study the efficacy by comparing ZD6474 in combination with Pemetrexed and Pemetrexed alone in 2nd line Non-small cell lung cancer patients and is expected to complete by December 2023.
  • Merck Sharp and Dohme LLC is conducting a Phase 3 clinical trial to study the efficacy and safety of Pemetrexed plus Platinum chemotherapy with or without Pembrolizumab (MK-3475) in patients with 1st line Metastatic Non-squamous Non-small cell lung cancer.

Molecule name

Number of studies

Folotyn (pralatrexate)


Pemfexy (pemetrexed)


Neutrexin (trimetrexate)


Otrexup (methotrexate)


Metoject (methotrexate autopen)



Target Indication Analysis of THF dehydrogenase Inhibitors

Drugs like Metoject (Methotrexate autopen) and Folotyn (pralatrexate) are commercially available THF dehydrogenase Inhibitors in the market and are used to treat various indications. Methotrexate is used for indications like Rheumatoid Arthritis, juvenile idiopathic arthritis, psoriasis, and various types of cancers like breast cancer, non-Hodgkin’s lymphoma and Crohn’s disease. Folotyn is an anti-neoplastic agent ad is used in the treatment of relapsed or refractory peripheral T-cell lymphoma. According to The Arthritis Foundation, the global prevalence of Rheumatoid Arthritis (RA) in developed countries is 0.5% to 1% with around 1.3 million people suffering from it in the USA in 2022. An increase in the incidence of RA is expected to create an opportunity and be a growth driver for the THF dehydrogenase Inhibitor market.

Frequently Asked Questions

Metoject (methotrexate autopen) and generic drugs like Methotrexate, Pemetrexed, Dapsone, and Atovaquone are some of the THF dehydrogenase Inhibitors approved by the FDA.

These are being used in various indications like Rheumatoid Arthritis, Malaria, Traveller’s diarrhea, multiple types of cancers like breast cancer and non-Hodgkin’s lymphoma, and others.

Nippon Medac, Aurobindo, Eagle Pharma, Pfizer, and Antares are some of the major market players for THF dehydrogenase Inhibitors.

Rising incidence of diseases, improvement in technologies, development of new treatment lines in the market and changing lifestyles leading to various types of cancers, and increasing incidence of RA are the key opportunities for THF dehydrogenase Inhibitors in the market.

Key Features of the Reports

  • The report provides granular level information about the market size, regional market share, historic market (2019-2023), and forecast (2024-2030)
  • The report covers in-detail insights about the competitor’s overview, company share analysis, key market developments, and their key strategies
  • The report outlines drivers, restraints, unmet needs, and trends that are currently affecting the market
  • The report tracks recent innovations, key developments, and start-up details that are actively working in the market
  • The report provides a plethora of information about market entry strategies, regulatory framework, and reimbursement scenario
  • Nippon Medac
  • Aurobindo
  • Eagle Pharma
  • Pfizer
  • Antares
  • Motif Bio
  • Syntrix
  • Azurity Pharma
  • Lirum Therap
  • Medicines for Malaria Venture
  • Aldeyra
  • MediQuest
  • Lundbeck
  • Pulmonem

Adjacent Markets