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Anaplerosis

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Pathways

TCA Cycle
Glycolysis
Electron Transport
β-Oxidation
Anaplerotic Input
Cataplerotic Exit
Amino Acid Input

What is Anaplerosis?

From Greek ana (up) + plerotikos (to fill). Anaplerosis is the replenishment of TCA cycle intermediates — the metabolic reactions that keep the engine running when its parts are consumed for other purposes.

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The Problem

TCA cycle intermediates are constantly being pulled away — for gluconeogenesis, amino acid synthesis, heme production, and fatty acid building. Without replenishment, the cycle stalls and energy production collapses.

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The Solution

Anaplerotic reactions feed new carbon skeletons back into the cycle. Pyruvate carboxylase (→ OAA), glutaminolysis (→ α-KG), and odd-chain fatty acid oxidation (→ succinyl-CoA) are the three major routes.

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The Medicine

Triheptanoin (Dojolvi®) is the first and only FDA-approved anaplerotic therapy. Its C7 fatty acid chains produce propionyl-CoA, which becomes succinyl-CoA — directly replenishing the cycle where it matters most.

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When It Breaks

TCA cycle enzyme deficiencies cause devastating neurological disease. But heterozygous loss of the same genes — SDH, FH, IDH — drives cancer through oncometabolite accumulation. The cycle connects rare disease to oncology.

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Every Breath

Two carbons enter each turn as acetyl-CoA. Two leave as CO₂ — becoming the air you exhale. The TCA cycle is why you breathe. It has been spinning in your cells since the moment you were conceived.

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Ancient

The TCA cycle predates oxygen in Earth's atmosphere. It likely ran in reverse in early anaerobic life, fixing CO₂ into organic molecules. It is one of the oldest metabolic pathways — perhaps 4 billion years old.

Eight Steps, One Turn

Each turn of the TCA cycle extracts the energy stored in acetyl-CoA's carbon bonds, capturing it as electron carriers (NADH, FADH₂) and direct energy (GTP), while releasing CO₂.

1

Oxaloacetate + Acetyl-CoA → Citrate

Citrate Synthase (CS)

The gateway reaction. A 4-carbon molecule grabs a 2-carbon fuel to form 6-carbon citrate.

Condensation
2

Citrate → Isocitrate

Aconitase (ACO2)

A molecular rearrangement via dehydration-rehydration. Aconitase's iron-sulfur cluster is sensitive to oxidative stress.

ACO2 deficiency
3

Isocitrate → α-Ketoglutarate

Isocitrate Dehydrogenase (IDH3)

First carbon exhaled as CO₂. First NADH captured. IDH mutations produce oncometabolite D-2-HG.

NADHCO₂IDH cancers
4

α-Ketoglutarate → Succinyl-CoA

α-KG Dehydrogenase Complex (OGDH/DLD)

Second CO₂ released. Another NADH. DLD is shared with PDH — one mutation disables both.

NADHCO₂DLD deficiency
5

Succinyl-CoA → Succinate

Succinyl-CoA Synthetase (SUCLA2/SUCLG1)

GTP born through substrate-level phosphorylation. This is where triheptanoin delivers its payload.

GTPmtDNA depletion
6

Succinate → Fumarate

Succinate Dehydrogenase / Complex II (SDHA/B/C/D)

The only enzyme in BOTH TCA and electron transport. SDH IS Complex II.

FADH₂SDH tumors
7

Fumarate → Malate

Fumarase (FH)

Biallelic FH loss = devastating IEM. Heterozygous = HLRCC with aggressive renal cancer.

FH deficiency / HLRCC
8

Malate → Oxaloacetate

Malate Dehydrogenase (MDH2)

The wheel completes. Final NADH captured. OAA is regenerated, ready for another turn.

NADHMDH2 deficiency

Net Yield Per Turn

3
NADH → ~7.5 ATP
1
FADH₂ → ~1.5 ATP
1
GTP → 1 ATP
2
CO₂ → exhaled

~10 ATP per turn · 2 turns per glucose · ~30–32 ATP total from oxidative phosphorylation

Anaplerotic Therapies

Therapies that replenish TCA cycle intermediates — from the only FDA-approved anaplerotic drug to investigational compounds.

L-Glutamine (Endari®)

FDA-approved for sickle cell disease

Glutamine → glutamate → α-ketoglutarate via GDH. Directly replenishes TCA. Dominant anaplerotic pathway in rapidly dividing cells and cancer.

→ α-Ketoglutarate

Odd-Chain Fatty Acids

C15:0 (pentadecanoic acid) · C17:0 (heptadecanoic acid)

Found in dairy fat and ruminant meat. β-oxidation yields propionyl-CoA → succinyl-CoA. Same mechanism as triheptanoin.

→ Succinyl-CoA

α-Ketoglutarate (AKG)

Ornithine-AKG · Calcium-AKG

Directly enters TCA as α-ketoglutarate. Used in burn patients and surgical recovery. Emerging interest in aging research.

→ α-Ketoglutarate

Branched-Chain FAs

dMC7 · AdMC7 · dMC9 · Investigational

Medium branched-chain fatty acids. Preclinical data shows improved TCA intermediate profiles vs. heptanoate in VLCAD/LCHAD/TFP/CPT-II fibroblasts.

→ Succinyl-CoA

Pyruvate Carboxylase

Endogenous enzyme · Biotin-dependent

The PRIMARY anaplerotic reaction: pyruvate + CO₂ + ATP → oxaloacetate. Allosterically activated by acetyl-CoA. When deficient, the entire TCA cycle starves.

→ Oxaloacetate

When the Cycle Breaks

TCA cycle enzyme defects cause some of the rarest and most severe inherited metabolic diseases. Partial loss of the same genes drives cancer — connecting rare disease to oncology.

SDH Tumor Syndromes

SDHA · SDHB · SDHC · SDHD · SDHAF2

Succinate accumulation inhibits α-KG-dependent dioxygenases, causing DNA hypermethylation and pseudo-hypoxia. Drives paraganglioma, pheochromocytoma, GIST, and renal cell carcinoma.

TCA Step: Succinate → Fumarate

IDH-Mutant Cancers

IDH1 (cytoplasmic) · IDH2 (mitochondrial)

Neomorphic mutations convert α-KG to D-2-hydroxyglutarate — an oncometabolite rewiring epigenetics. Found in >70% of low-grade gliomas, ~20% of AML. FDA drugs: ivosidenib, enasidenib, vorasidenib.

TCA Step: Isocitrate → α-Ketoglutarate

Fumarase Deficiency / HLRCC

FH · OMIM 606812

Biallelic: severe encephalopathy, fumaric aciduria. Heterozygous: hereditary leiomyomatosis + aggressive type 2 papillary RCC. Fumarate = oncometabolite.

TCA Step: Fumarate → Malate

Succinyl-CoA Ligase Deficiency

SUCLA2 · SUCLG1 · OMIM 612073 / 245400

SUCLA2: encephalomyopathy with mtDNA depletion and methylmalonic aciduria. SUCLG1: fatal infantile lactic acidosis. The link between the TCA cycle and the mitochondrial genome.

TCA Step: Succinyl-CoA → Succinate

Pyruvate Carboxylase Deficiency

PC · OMIM 266150

Three types: Type A (infantile), Type B (neonatal, severe), Type C (benign). When the primary anaplerotic enzyme fails, OAA cannot be replenished, gluconeogenesis halts.

Anaplerotic Input: Pyruvate → Oxaloacetate

LC-FAOD Spectrum

ACADVL · HADHA · HADHB · CPT1A · CPT2 · SLC25A20

VLCAD, LCHAD, TFP, CPT-I/II, CACT. Cannot generate acetyl-CoA from long-chain fats. TCA intermediates deplete. Triheptanoin (Dojolvi) is FDA-approved for these conditions.

TCA Impact: Acetyl-CoA + anaplerotic depletion