Sarecycline Hydrochloride (Syn: Sarecycline HCl) is the hydrochloride salt of Sarecycline, a narrow-spectrum antibiotic belonging to the tetracycline class. It is a modified derivative of naturally occurring tetracyclines. Unlike other tetracyclines, Sarecycline has a long C7 moiety that directly interacts with the bacterial messenger RNA. The compound was discovered by Paratek Pharmaceuticals (Boston, MA). It can be used to study acne vulgaris.
Sarecycline HCl is soluble in DMSO.
| Mechanism of Action | Sarecycline HCl binds to the A site of the bacterial 30S subunit of the bacterial ribosome. This blocks the attachment of aminoacyl-tRNA molecules to the ribosome, which is necessary for the addition of new amino acids to the growing polypeptide chain. This leads to the inhibition of bacterial protein synthesis. |
| Spectrum |
Sarecycline is active against Gram-positive bacteria, mainly Cutibacterium with minimal activity against aerobic Gram-negative bacteria. Sarecycline exhibits antibacterial activity against important skin/soft tissue pathogens with targeted activity against Cutibacterium acnes--an anaerobic Gram-positive bacterium linked with acne lesions. Also active against tetracycline-resistant Staphylococcus aureus as well as erythromycin- and clindamycin-resistant C. acnes strains |
| Microbiology Applications |
Sarecycline has antibacterial activity against the bacteria causing acne vulgaris (Cutibacterium acnes). It has activity against inflammatory lesions of non-nodular moderate to severe acne vulgaris. Acne vulgaris is a chronic skin condition associated with the blockage and/or inflammation of hair follicles and their sebaceous glands. Sarecycline has a low propensity for resistance development in these pathogens and a narrower spectrum of activity. In vitro evaluation of 55 clinical isolates of Cutibacterium acnes were inhibited. MIC values range: 0.5 - 16 µg/ml; MIC50: 0.5 µg/ml; MIC90: 4 µg/ml (Zhanel et al, 2018). |
| Eukaryotic Cell Culture Applications |
Human bone marrow-derived mesenchymal stromal cells (hBMSCs) were exposed to a concentration range of Sarecycline to review its metabolic activity, morphology and osteoblastic differentiation capability in vitro. Authors were reviewing the modulation of Wnt, Hedgehog, and Notch signaling pathways. They found hBMSCs cultured with this compound had increased metabolic activity compared to the control, with an indistinguishable cell morphology. They concluded that Sarecycline is a strong candidate for drug repurposing studies for the enhancement of bone healing/regeneration (Martin et al, 2023). |
| Molecular Formula |
C24H29N3O8·HCl |
| References |
Kaul G, Saxena D, Dasgupta A, Chopra S (2019) Sarecycline Hydrochloride for the treatment of acne vulgaris. Drugs Today (Barc). 55(10):615-625 PMID 31720559 Martin V, Grenho L, Fernandes MH, Gomes PS (2023) Repurposing Sarecycline for osteoinductive therapies: An in vitro and ex vivo assessment. J Bone Miner Metab 41:431–442 Zhanel G, Critchley I, Lin LY, Alvandi N (2018) Microbiological profile of Sarecycline, a novel targeted spectrum tetracycline for the treatment of Acne vulgaris. Antimicrob Agents Chemother.;63(1):e01297-18 PMID 30397052 |
