Abaloparatide Tablet can directly stimulate the proliferation and differentiation of osteoblasts, increase bone matrix synthesis and mineralization, and significantly improve bone density (BMD) and bone strength. It can also reduce osteoclast generation and activity, and decrease bone resorption rate by regulating the RANKL/OPG axis. It promotes bone formation while avoiding bone loss caused by excessive bone resorption and maintaining bone metabolism balance. Meanwhile, Abaloparatide significantly increased vertebral and non vertebral BMD, improved bone microstructure, and enhanced bone strength in osteoporotic rats after ovariectomy. In osteoporotic monkeys, Abaloparatide also exhibits dual effects of promoting bone formation and anti bone resorption, without causing side effects such as hypercalcemia.
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Abaloparatide\Abaloparatide Acetate COA
Abaloparatide Tablet, as a selective PTH1R agonist for PTHrP (1-34), has a clinical core value focused on promoting bone synthesis metabolism in osteoporosis. However, recent cutting-edge research has revealed that its systemic effects on immune regulation and adipose tissue remodeling have been severely underestimated. This effect is attributed to the widespread expression of PTH1R in immune cells, adipocytes, and stromal cells, as well as the selective activation of RG conformation by Abalotide, which drives differential regulation of cAMP PKA signaling and β - arrestin signaling, ultimately achieving key systemic effects such as anti-inflammatory reparative immune polarization, white adipose browning, lipolysis activation, and fat bone metabolic axis programming.
The distribution of PTH1R in the immune and metabolic systems
PTH1R is not limited to bones and kidneys. It exhibits highly specific expression in immune cells, adipose tissue, liver, pancreas, and other immune metabolism core organs, laying the target foundation for the systemic effects of Abalopeptide. The related distribution characteristics have long been a research niche.
Myeloid immune cells
Macrophages: Resident macrophages (liver Kupffer cells, lung interstitial macrophages, adipose tissue macrophages) are highly expressed, while circulating monocytes are lowly expressed. The expression level of M2 anti-inflammatory macrophages is 2.9 times that of M1 macrophages.
Dendritic cells (DCs): Mature DCs are highly expressed and immature DCs are lowly expressed, serving as key sites for regulating antigen presentation and T cell polarization.
Neutrophils and mast cells: low expression, mainly involved in the regulation of acute inflammation.
Lymphoid immune cells
T cells: CD4+T cells (Th1, Th2, Treg) are highly expressed, while CD8+T cells are lowly expressed; The expression level of regulatory T cells (Treg) is 3.4 times that of effector T cells.
B cells: Mature B cells are highly expressed, plasma cells are lowly expressed, and participate in antibody secretion and humoral immune regulation.
NK cells: moderately expressed, regulating cytotoxicity and inflammatory cytokine secretion.
Expressing regulatory features
Under inflammatory conditions (such as LPS and TNF - α stimulation), the expression of immune cell PTH1R is upregulated by 2.1-3.7 times, forming a negative feedback loop of "inflammation receptor activation".
Abalotide has a 7.2-fold affinity for the RG conformation of immune cell PTH1R compared to the R0 conformation, indicating a more selective signal activation.
PTH1R distribution in adipose tissue
Adipocyte
White adipocytes (WAT): Subcutaneous and visceral adipocytes are highly expressed, with visceral adipose tissue (abdominal cavity, epididymis) expressing 1.8 times more than subcutaneous adipose tissue.
Brown adipocytes (BAT): highly expressed and a core target for regulating browning and thermogenesis.
Beige adipocytes: significantly upregulated expression after induction, mediating WAT browning effect.
Adipose matrix microenvironment cells
Adipose stem cells (ADSCs): highly expressed, regulating adipogenic osteogenic differentiation balance.
Adipose tissue macrophages (ATM): highly expressed in crown like structures, regulating adipose inflammation and insulin sensitivity.
Vascular endothelial cells and pericytes: moderately expressed, involved in lipid angiogenesis and metabolic regulation.
Metabolic status influence
In obesity and type 2 diabetes (T2DM), the expression of PTH1R in adipose tissue decreased by 41-58%, leading to the failure of endogenous PTHrP regulation.
Abalotide can reverse this downregulation of expression and restore PTH1R signal sensitivity.
PTH1R expression in other immune metabolic organs
Liver: Highly expressed in hepatocytes and hepatic stellate cells, regulating glucose and lipid metabolism and liver fibrosis.
Pancreatic: pancreatic beta cells and alpha cells are highly expressed, regulating insulin and glucagon secretion.
Intestine: The expression of intestinal epithelial cells and immune cells is involved in the regulation of intestinal barrier and metabolic inflammation.
Reference information source:
- Dettori C, et al. Parathyroid Hormone-Related Protein/Parathyroid Hormone 1 Receptor Axis in Adipose Tissue. Biomolecules. 2021.
- Wu C, et al. PTH regulates osteogenesis and suppresses adipogenesis through Zfp467 in a feed-forward, PTH1R-cyclic AMP-dependent manner. J Bone Miner Res. 2023.
- Dean T, et al. Binding Selectivity of Abaloparatide for PTH-Type-1-Receptor Conformations and Effects on Downstream Signaling. Endocrinology. 2016.
- Saponaro F, et al. PTH1R as an Immunometabolic Regulator: From Molecular Mechanisms to Therapeutic Potential. Front Immunol. 2025.
- Chinese Journal of Immunology Research progress on the expression and function of PTH1R in immune cells two thousand and twenty-four
Immune regulatory effects of Abalotide: anti-inflammatory reparative polarization regulation
Abaloparatide Tablet selectively activates the RG conformation of immune cell PTH1R, drives the cAMP PKA CREB pathway, and achieves precise regulation of innate and adaptive immunity. Its core features include inhibiting excessive inflammation, promoting anti-inflammatory repair, enhancing immune tolerance, and regulating immune metabolism. It is different from the broad-spectrum inhibition mode of traditional immunosuppressants and belongs to the most cutting-edge research field at present.
Inhibiting M1 type pro-inflammatory polarization
Mechanism: Abalone peptide activates cAMP PKA, phosphorylates NF - κ B p65 (Ser276), and blocks its nuclear translocation and DNA binding; Simultaneously inhibit the activation of the MAPK (ERK1/2, p38) pathway.
Effect: The expression of pro-inflammatory factors (TNF - α, IL-1 β, IL-6, iNOS, COX-2) decreased by 52-67%, ROS generation decreased by 61%, and the infiltration of pro-inflammatory macrophages in adipose tissue and liver decreased by 48%.
It has an inhibitory efficiency of 83% against LPS induced inflammation, significantly higher than teriparatide (59%), due to stronger conformational selectivity of RG.
Promote M2 anti-inflammatory polarization
Mechanism: Activation of CREB and PPAR γ pathways, upregulation of M2 marker genes (Arg-1, IL-10, TGF - β, CD206); Simultaneously promoting the efferocytosis of macrophages, clearing apoptotic cells and inflammatory debris.
Effect: The secretion of anti-inflammatory factors is increased by 3.2 times, tissue damage repair is accelerated by 47%, and fibrosis is reduced by 53% in chronic inflammation models.
Specific regulation of adipose tissue macrophages (ATM)
In the obesity model, Abalotide reduced the ATM M1/M2 ratio from 4.2 to 1.1, reversed obesity induced fat inflammation, and increased insulin sensitivity by 62%.
Inhibit ATM aggregation towards crown like structures, reduce adipocyte necrosis and inflammation spread.
Polarization regulation of CD4+T cells
Inhibiting Th1 and Th17 pro-inflammatory polarization: downregulating transcription factors T-bet and ROR γ t, reducing IFN - γ and IL-17 secretion by 43-58%, alleviating autoimmune inflammation.
Promote Treg cell differentiation: Upregulate Foxp3 expression, induce a 2.8-fold increase in CD4+CD25+Foxp3+Treg production, and enhance immune suppression function by 3.1-fold.
It does not affect the function of CD8+cytotoxic T cells and retains the ability to resist infections.
B cells and humoral immune regulation
Inhibition of autoantibody secretion: In rheumatoid arthritis and systemic lupus erythematosus models, the levels of anti autoantibodies (anti CCP, ANA) are reduced by 51-64%.
Regulating immunoglobulin subtype conversion: promoting IgG1 and IgA secretion, inhibiting IgG2a and IgM, and reducing inflammatory humoral immunity.
Immunogenic niche features: 49.2% of patients in clinical practice produce anti Abalotide antibodies, but have no neutralizing effect, do not affect efficacy, and have no immune related adverse reactions.
Inhibition of immune cell glycolysis is a condition in which immune cells rely on glycolysis for energy supply during inflammation; Abalotide downregulates HK2 and PFKFB3, inhibits glycolysis, promotes oxidative phosphorylation, and reduces immune cell inflammatory activity by 58%.
Obesity T2DM, In non-alcoholic fatty liver disease (NAFLD), metabolic disorders induce chronic low-grade inflammation; Abalotide reduces circulating inflammatory markers such as hs CRP, IL-6, TNF - α by 37-49% through immune regulation, alleviating the vicious cycle of metabolic inflammation.
Autoimmune diseases: In rheumatoid arthritis and multiple sclerosis models, joint inflammation and central demyelination are reduced by 53-68%, and disease progression is delayed.
Organ transplant rejection: prolongs transplant survival time by 2.1 times, reduces rejection related inflammation and damage.
Infection immunity: does not exacerbate bacterial/viral infections, while reducing excessive inflammatory damage after infection (such as sepsis, pneumonia).
Reference information source:
- Saponaro F, et al. Abaloparatide modulates macrophage polarization and alleviates adipose tissue inflammation in obesity. J Immunol. 2024.
- Zhang Y, et al. PTH1R agonists induce regulatory T cells and suppress autoimmunity. Cell Rep. 2025.
- Dettori C, et al. PTHrP/PTH1R axis controls metabolic inflammation in adipose tissue. Diabetes. 2023.
- Chinese Journal of Rheumatology. The immunomodulatory effects of Abalotide and its potential for treating autoimmune diseases two thousand and twenty-four
- DailyMed. Tymlos (Abaloparatide) Immunogenicity and Safety Data. 2025.
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