Drug General Information
Drug ID	D00FGR
Drug Name	Miltefosine
Synonyms	HDPC; HePC; Hexadecylphosphocholine; Hexadecylphosphorylcholine; Impavido; Miltefosina; Miltefosinum; Miltex; Baxter Oncology brand of miltefosine; Baxter brand of miltefosine; Miltefosin C; Prasfarma brand of miltefosine; D 18506; IN1227; D-18506; H-1850; M-7200; Miltefosina [INN-Spanish]; Miltefosine (INN); Miltefosine[INN:BAN]; Miltefosinum [INN-Latin]; N-Hexadecylphosphorylcholine; TF-002; Choline hydroxide, hexadecyl hydrogen phosphate, inner salt; Choline, hexadecyl hydrogen phosphate, inner salt; Hexadecyl 2-(trimethylazaniumyl)ethyl phosphate; Choline phosphate, hexadecyl ester, hydroxide, inner salt; Choline phosphate, hexadecyl ester, hydroxide, inner salt (6CI); Hexadecyl 2-(trimethyl-.lambda.~5~-azanyl)ethyl hydrogen phosphate; Ethanaminium, 2-(((hexadecyloxy)hydroxyphosphinyl)oxy)-N,N,N-trimethyl-, hydroxide, inner salt; Ethanaminium, 2-(((hexadecyloxy)hydroxyphosphinyl)oxy)-N,N,N-trimethyl-, hydroxide, innner salt; 1-Hexadecylphosphorylcholine; 2-(((Hexadecyloxy)hydroxyphosphinyl)oxy)-N,N,N-trimethylethanaminium hydroxide, inner salt; 3,5-Dioxa-4-phosphaunacosan-1-aminium, 4-hydroxy-N,N,N-trimethyl-, hydroxide, inner salt, 4-oxide
Drug Type	Small molecular drug
Therapeutic Class	Antifungal Agents
Company	Aeterna Zentaris
Structure
Drug Resistance Mutations
Target Name	Parasitic Phospholipid-transporting ATPase (LdMT)				Target Info
Gene Name	LdMT
Uniprot ID	Q6VXY9_LEIDO
Species	Leishmania donovani
Reference Sequence	MPNQPPCWRKCLSTRIFPDKLSKSFCCFSAEADVDEDDEVIVYLNDPELNAQFNYPSNFI RTSKYTLISFLPLSLLLEFKKVSNLYFLMNVIFSLIPGVSPLSPATSIAPLSFVLIVALI KEGVEDIKRHQADNRANSILVQVLRNGKLVSVHSKDIHPGDVMRIKNGEEVRADVVMLAS SVEEGQAFIDTCNLDGETNLKSRKALEATWALCEVEAIMNSTAVLHTSKPDPGLLSWAGL LEINGEEHALSLNQFLYRGCVLRNTDWVWGMVAYAGVDTKLFRNLKPKPPKSSNLDRKLN YFIIAILIFQNIMLFILASMAVWWNSKYRETPYLRFFISFRKNVTLWGYRYLSYFILLSY CVPISLFITIEVCKVVQAQWMRVDCLMMEYMSNRWRHCQPNTSNLNEQLAMVRFIFSDKT GTLTENVMKFKLGDALGNPIDADNLDECIAQLRKEAESKGLGPLQEYFLALALCNTVQPF KDDTDDLGVVYEGSSPDEVALVETAAAVGYRLISRTTKSITLLLHDGTRKVYNILATLEF TPDRKMMSIIVEDSDTKKITLYNKGADSFIRPQLSRAPDVQGHIENVEIPLTEMSSSGLR TLLVCAKDITRRQFDPWFEKFVEAGKSLHNRSSNIDKVCLEMEQDMRLVGATAIEDKLQD EVPETLSFFLSAGVIIWMLTGDKRETAVTIAATSTLCDPRNDFIDHIDIGHLNSSDPKAI ERVGRDLEVVEQHIALKGTHKERRCTLVIDGPALNIAMEHYFDQFLRLSHQVNSAVCCRL TPIQKATVVRMFQKSTGKTALAIGDGANDVSMIREGRVGVGIIGLEGAHAALAADYAIPR FKHLRRLCAVHGRYSLFRNASCILVSFHKNITVSVVQFIFAFYVGFSGLTLFDGWMLTFY NVLLTSIPPFFMGIFDKDLPEDALLERPKLYTPLSHGEYFNLATLLRWFVESLTTAVILF YAAYPTLIRQDGSHQRYTGGETGTLVFSGLILVIQTRFILQIRYWQWLQVFGMAMSIFLF LLLFLVYSAIPSVFSDTNFYYQAFDLMSTAKYWFFLLLYVGTEVVVVLGVMTFQKNLFPT LRDVAERQYAVQNGGKL [Leishmania donovani]
Targeted Disease	Leishmaniasis
Drug Resistance Mutations	Mutation info Missense: M381T [1], [2]
	Mutation info Missense: F1078Y [2]
Target Name	Parasitic Phospholipid-transporting ATPase (Ros3)				Target Info
Gene Name	Ros3
Uniprot ID	Q0P0L8_LEIDO
Species	Leishmania donovani
Reference Sequence	MAPLPPKPHSKNRIEQQQLPHIYARHSPLSVSVVFFILAVAAIPIGVLVIVSGDLTTRLD FRYDHINSYKFAMGAAGEFAVNFPFNGTMYSSGVKTRLMFSLHQSLTAPVYMQYRLSPFF QNYRYFTASVDYSQLSGRASAISKLCAPFRFPGEATGDSVSGYYNPCGAYPWAMFNDSIS LYRTDGTLICDGSAFTANGTSLAANNKCVKSGIARPSDVKERYNPPREIPGNGPMWSAGG NKSATDPYLREGYYYKEPGHKIPLSIDEDLIVWLDPAFTSDVTKNYRILNVDLPAGDYYF EITEQYPTAPYASHKFVQLATRSWIGGRSHVLGSLLIIMGGTAFIMAVTLLSVKYLIMPV YTEDI [Leishmania donovani]
Targeted Disease	Leishmaniasis
Drug Resistance Mutations	Mutation info Missense: Y354F [2]
Target Name	Fungal Metacaspase-1 (MCA1)				Target Info
Gene Name	MCA1
Uniprot ID	MCA1_YEAST
Species	Saccharomyces cerevisiae
Reference Sequence	MYPGSGRYTYNNAGGNNGYQRPMAPPPNQQYGQQYGQQYEQQYGQQYGQQNDQQFSQQYA PPPGPPPMAYNRPVYPPPQFQQEQAKAQLSNGYNNPNVNASNMYGPPQNMSLPPPQTQTI QGTDQPYQYSQCTGRRKALIIGINYIGSKNQLRGCINDAHNIFNFLTNGYGYSSDDIVIL TDDQNDLVRVPTRANMIRAMQWLVKDAQPNDSLFLHYSGHGGQTEDLDGDEEDGMDDVIY PVDFETQGPIIDDEMHDIMVKPLQQGVRLTALFDSCHSGTVLDLPYTYSTKGIIKEPNIW KDVGQDGLQAAISYATGNRAALIGSLGSIFKTVKGGMGNNVDRERVRQIKFSAADVVMLS GSKDNQTSADAVEDGQNTGAMSHAFIKVMTLQPQQSYLSLLQNMRKELAGKYSQKPQLSS SHPIDVNLQFIM [Saccharomyces cerevisiae]
Targeted Disease	Leishmaniasis
Drug Resistance Mutations	Mutation info Missense: N164D [3]
References
REF 1	CRISPR-Cas9-Mediated Genome Editing in Leishmania donovani. MBio. 2015 Jul 21;6(4):e00861.
REF 2	Laboratory confirmed miltefosine resistant cases of visceral leishmaniasis from India. Parasit Vectors. 2017 Jan 31;10(1):49.
REF 3	Functional disruption of yeast metacaspase, Mca1, leads to miltefosine resistance and inability to mediate miltefosine-induced apoptotic effects.Fungal Genet Biol.2014 Jun;67:71-81.

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